May 27-29, 2011 WOW Topkapı Palace Antalya-TÜRKİYE

Organized by Hacettepe University Medicinal Chemistry Research Development & Application Center ABSTRACTS www.drd.hacettepe.edu.tr Dear Colleagues,

I would like to invite you to attend and contribute to the International Symposium on Drug Research and Development “From Chemistry to Medicine” DRD 2011 and New Horizons and Job Opportunities for Young Scientists which is organized by Hacettepe University, Medicinal Chemistry Research, Development and Application Center (MAGUM).

MAGUM, a subunit of Hacettepe University, was established in 1996 for the purpose of realization of the drug design, structure-activity relationships, synthesis, analysis and molecular quality control of synthetic and natural drugs and drug raw materials in medicinal chemistry area with cooperation of departments of Faculty of Pharmacy, Faculty of Medicine and other facul- ties to improve outputs of drug research, development and application by multidisciplinary collaboration approaches.

The high quality performed scientific International Symposium on Drug Research and Development “From Chemistry to Medicine” organized by MAGUM every two years. In addition to DRD 2011 symposium, which will be held on May 27-29, 2011, New Horizons and Job Opportunities for Young Scientists” was also planned to conduct by MAGUM.

The mission of “International Symposium DRD 2011 and New Hori- zons and Job Opportunities for Young Scientists” will be to provide a scientific forum by the invitation of distinguished scientists having national / international reputation in their areas, so the most recent advances will be discussed and evaluated interactively and the exchange of interdisciplinary knowledge from chemistry to medicine. The format of the scientific program will also include oral and poster presentations on the concerning scientific topics in addition to the invited lectures.

Members of the organizing committee and I cordially invite you to join us at DRD 2011 in Antalya, May 27-29, 2011. It is important to note that symposium venue Antalya is very famous with its archaeological and natural riches and known as one of the most popular region of Turkish Riviera.

We are looking forward to see you in Antalya,Turkey. With our kind regards,

Prof. Dr. Ünsal ÇALIŞ Chair ORGANIZING COMMITTEE Honorary Chair Prof. Uğur ERDENER, M.D. President of Hacettepe University Organizing Committee Ünsal ÇALIŞ, Ph.D. (Chair) Selma SARAÇ, Ph.D. Sedef KIR, Ph.D. Gülberk UÇAR, Ph.D. Funda Nuray YALÇIN, Ph.D. S. Kutay DEMİRKAN, Pharm.D.

ADVISORY BOARD Prof. Melih ALTAN, Ph.D. (Ankara University, Türkiye) Prof. Metin BALCI, Ph.D. (Middle East Technical University, Türkiye) Prof. Erden BANOĞLU, Ph.D. (Gazi University, Türkiye) Prof. A. Ahmet BAŞARAN, Ph.D. (Hacettepe University, Türkiye) Prof. Erdem BÜYÜKBİNGÖL, Ph.D. (Ankara University, Türkiye) Prof. Sevim DALKARA, M.D. (Hacettepe University, Türkiye) Prof. Katerina GORACINOVA, Ph.D. (University of Sts Cyrill and Methodius, Macedonia) Prof. Arzum Erdem GÜRSAN, Ph.D. (Ege University, Türkiye) Prof. Selçuk GEÇİM, Ph.D. (Hacettepe University, Türkiye) Prof. Emin KANSU, M.D. (Hacettepe University, Türkiye) Prof. Hakan ORER, M.D. (Hacettepe University, Türkiye) Prof. Seçkin ÖZDEN, Ph.D. (Ankara University, Türkiye) Prof. Yekta ÖZER, M.D. (Hacettepe University, Türkiye) Prof. Serhat ÜNAL, M.D. (Hacettepe University, Türkiye) Prof. Metin TÜLÜ, Ph.D. (Yıldız Technical University, Türkiye) Prof. Kemal YELEKÇİ, Ph.D. (Kadir Has University, Türkiye) Prof. Nurşen ÜNLÜ, Ph.D. (Hacettepe University, Türkiye)

SCIENTIFIC SECRETERIAT OFFICIAL SYMPOSIUM AGENCY

Prof. Selma SARAÇ, Ph. D. DMR Congress Organization Services Tourism Inc. Hacettepe University, Faculty of Pharmacy Hollanda Cad. 696. sok. 22/9-10 Department of Pharmaceutical Chemistry 06550 Yıldız Çankaya - Ankara, TURKEY 06100 Ankara-TÜRKİYE Phone : +90 312 442 01 50 Phone (Fax) : +90 312 305 30 15 Fax : +90 312 442 04 10 [email protected] www.dmrturizm.com.tr [email protected] Prof. Sedef KIR, Ph. D. Hacettepe University, Faculty of Pharmacy Department of Analytical Chemistry 06100 Ankara-TÜRKİYE Phone : +90 312 305 21 63 [email protected]

CONTENTS 6 10 11 13 39 53 166 5

DRD 2011 DRD

International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International SCIENTIFIC PROGRAMME SPONSORS EXHIBITION LECTURES ORAL PRESENTATIONS POSTER PRESENTATIONS ındex SCIENTIFIC PROGRAMME 10.30-11.00 09.00-10.30 MAY 28,2011 18.00-20.00 16.30-18.00 16.00-16.30 16.00-16.30 14.30-16.00 MAY 27,2011 Coffee Break Woei PingCheng,University ofHertfordshire, United Kingdom Improving Treatment ofDiseases Novel Nano-carriers BasedonSelf-assembling Polymers: ANew Opportunityfor Katerina Goracinova, University ofStsCyrillandMethodius,Macedonia Colloidal Carriers for Anticancer DrugDelivery –Formulation Approaches Nils Rottmann,BASF-TheChemical Company, Germany Novel Excipients from Scratch to Launch Sema Çalış,Hacettepe University, Türkiye Nurşen Ünlü,Hacettepe University, Türkiye Chairpersons : (All presentations willbeinEnglish) Delivery Systems Current Approaches for Development ofNovel Drug SESSION II WELCOME RECEPTIONSponsored by Arzum Erdem Gürsan, EgeUniversity, Türkiye DNA Interactions Nanomaterial BasedSensorTechnology for Electrochemical Monitoring Drug- Kemal Yelekçi, KadirHasUniversity, Türkiye Inhibitors: Evaluation ofComputational andExperimental InhibitionValues In Silico DesignofNovel andHighly Selective MonoamineOxidaseAandB Farhad Farshi, Abdiİbrahim Pharmaceutical R&DCenter, Türkiye New Trends inPharma:TheGrowth ofGenerics Nur Onar, OndokuzMayısUniversity, Türkiye Cyprus Rümeysa Demirdamar, NearEast University, Turkish RepublicofNorthern Chairpersons : (All presentations willbeinEnglish) Development New Trends andMethodsinDrugResearch and SESSION I Coffee Break Coffee Break Firas El-Saleh, ISP-International SpecialtyProducts, Germany The UseofNovel EnablingTechniques to Overcome DrugSolubilityIssues Woei PingCheng,University ofHertfordshire, United Kingdom Engineering Versatile Nano-carriers for Therapeutic Delivery Opening Lectures OPENING CEREMONY International Symposium onDrugResearch &Development 2011 DRD 2011 6 Sponsored by Sponsored by SCIENTIFIC PROGRAMME SCIENTIFIC PROGRAMME İLADER Supported by Supported 7 DRD 2011 DRD Federal Urdu University of Arts, Pakistan Arts, of University Urdu Federal Pakistan International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International SESSION III-A SESSION Agents Clinicians: Diabetic of Expectations and Experiences Turkish) will be in (All presentations Chairperson: Türkiye University, Hacettepe Gülberk Uçar, of Administration & Routes Insulin Therapy Türkiye Uludağ University, Tuncel, Ercan Diabetic Therapy Oral Türkiye University, Başkent Demirağ, Nilgün Güvener Agents Antidiabetic New Türkiye University, Okan Yıldız, Hacettepe Bülent LUNCH III-B SESSION in Pharmaceutical and Development on Research Presentations Oral Selected Sciences will be in English) (All presentations : Chairpersons Türkiye Ege University, Gürsan, Arzum Erdem Macedonia of Sts Cyrill and Methodius, University Goracinova, Katerina and Non-polarized Live in Trafficking Endosomal and Entry Reovirus Monitoring Tracking 4,5-Dimethyl-1,3,4,5- Particle Viral of Single by Cells Polarized Interconversion Conformational School, USA Medical Harvard Cömert Kural, the of Study Computational through tetrahydro-2H-1,5-benzodiazepin-2-one Samples Important Biologically Austria University, Karl Franzens Some Sajid Jahangir, of Activity Antioxidant of Determination Voltammetry Cyclic and Technology, of Arts, Science University Urdu Haji Muhammad, Federal Technetium- with Radiolabelling Conjugate, Folate-PEG-Doxorubicin of Synthesis Cancer in Agent Imaging an as Applications its into Research and 99m Türkiye Güliz Ak, Ege University, Extract of Grapefruit Study the Effects Used to Bioengineering Technique Parameters Emulsion on Human Skin Mechanical Containing Spp, Pakistan Fasciola of Bahawalpur, The Islamia University Akhtar, Naveed against Efficacy Combination Anthelmentic Iran Commercial a Urmia, on in Study Ruminants Small in Spp Moniezia and Dendriticum Dicrocoelium Iran Rasouli, Islamic Azad University, Sohrab Water Waste by Industrial Irrigated in Root Vegetables Toxicity Heavy Metals Karachi Yasmeen, Kousar and of Mulberry Extract Creams Bleach of Two and Characterization Formulation on Human Skin Melanin and Erythema Comparison of their Effects of the Punjab, Pakistan The University Rasool, Fatima Lunch & Exhibition Discussion Poster 12.30-14.00 14.00-14.30 11.00-12.30 12.30-14.00 11.00-12.30 SCIENTIFIC PROGRAMME 20:00-24:00 16.30-18.00 16.00-16.30 14.30-16.00 Gala Dinner Sami Türkoğlu, UlkarHolding,Türkiye Farhad Farshi, Abdiİbrahim Pharmaceutical R&DCenter, Türkiye A.Tuncay Teksöz, PfizerInc.Pharmaceutical Company, Türkiye The Scientific& Technological Research Councilof Türkiye- TÜBİTAK Emel ÖnderFırat Tuğba Arslan Kantarcıoğlu, TheScientific& Technological Research Rıza Alagöz, Murat Yıldız, Tayfun Öner, Small&MediumEnterprises Development Organization Tarık Çelik,TheTurkish Academy ofSciences TÜBA,Türkiye Selçuk Geçim,Hacettepe University, Türkiye Moderator : (All presentations willbeinTurkish) New Horizons and JobPANEL Opportunities for Young ScientistsCoffee Break &Exhibition A. AtillaHıncal, İDEPharmaceutical Consultancy, Türkiye Development Requirements ofScientificBackground for JobApplications inDrugResearch and Aykut Bora, BilimPharmaceutical Company, Türkiye Personal Behaviors DuringJobInterview Nesrin Dilbaz, Getting Readyfor Interview andGetOver Your Fear Buket Aksu,Santa Farma Pharmaceutical Company, Türkiye Chairperson : (All presentations willbeinTurkish) Interview Fear inJobApplications SESSION IV International Symposium onDrugResearch &Development 2011 Republic of Turkey Ministry of Industry and Trade, Türkiye KOSGEB, Türkiye Republic of Turkey Ministry of Industry and Trade, Türkiye Ankara Numune Research And Training Hospital, Türkiye CouncilofTürkiye- TÜBİTAK DRD 2011 8 Supported by İLADER SCIENTIFIC PROGRAMME Sponsored by Sponsored Sponsored by Sponsored Sponsored by Sponsored

9 DRD 2011 DRD International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Inserm Institut, France Inserm Institut, Parini, Angelo Function Cardiovascular of Control Serotonergic France of Toulouse, Nathalie Pizzinat, University Break Coffee VI SESSION of Pharmaceutical and Analysis Synthesis Organic Molecules will be in English) (All presentations : Chairpersons Türkiye Özden, Gazi University, Tuncel Türkiye University, Ankara Büyükbingöl, Erdem Heterocycles the Synthesis of Various for Milestone Bisacylazides: A New Türkiye University, Technical East Middle Metin Balcı, Synthesis of Pamam Microwave-Assisted Drug Carriers: as Potential Dendrimers Dendrimers Type Türkiye University, Yıldız Technical Metin Tülü, its Preparation for Process Acid and of Zoledronic Polymorph A Novel Holding API R&D, Türkiye Bekir Karlığa, Deva Absorption Inhibitor Cholesterol Synthesis of Ezetimibe: A Selective Holding API R&D, Türkiye Esen Bellur Atıcı, Deva Lunch SEARCH CONFERENCE of Drug R & D: Visualising the Future Priorities and Strategies Policies, will be in Turkish) (All presentations Moderator: Türkiye Consultant, İsmail Üstel, Remarks Closing SESSION V SESSION Drug Development to Approaches Biochemical Recent will be in English) (All presentations : Chairpersons Türkiye University, Ankara Zeliha Büyükbingöl, Türkiye University, Hacettepe Filiz Hıncal, in Top2 Targeting of Mechanisms Agent: Cytotoxic a into Enzyme an Change to How Cancer Enhanced Memphis-USA Hospital, Research St. Jude Children’s John L. Nitiss, on Impact Cells: Stem Mesenchimal Marrow Bone of Activity Paracrine and Survival Syndromes Ischemic of Therapy Cell 10.30-11.00 11.00-12.30 12.30-14.00 14.00-16.00 16.00-16.30 09.00-10.30 MAY 29, 2011 29, MAY SPONSORS International Symposium onDrugResearch &Development 2011 DRD 2011 10 SPONSORS EXHIBITION EXHIBITION EXHIBITION AREA HALL A HALL B POSTER MEETING MEETING 11 DRD 2011 DRD ISP 5 4 7 6 9 8 INNOVA REDOKS İNCEKARA International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International MEDSANTEK LABOR İLDAM LABOR

STAND AREA STAND

BAS-F 3

2 1 ANAMED ANT TEKNİK ANT

LECTURES

DRD 2011 LECTURES I-01 ENGINEERING VERSATILE NANO-CARRIERS FOR THERAPEUTIC DELIVERY Woei Ping CHENG School of Pharmacy, University of Hertfordshire, College Lane, Hatfield, UK AL10 9AB [email protected]

oday with the advancement of biotechnology, a Addition of quaternary ammonium moieties onto these plethora of new therapeutic macromolecules such as self-assembled polymers have protected insulin and sCT Tproteins/peptides and siRNA have been discovered against in vitro enzymatic degradation1,2 and enhanced to treat a variety of diseases ranging from cancer, autoim- the uptake of these complexes by CaCO2 cells via trans- mune diseases to metabolic diseases. Albeit their huge cellular and paracellular pathways4. In vivo study using je- potentials, one of the major hurdles has yet to overcome is junal instillation has demonstrated the feasibility of using drug delivery problem. Unlike small drug molecules, these these nano-complexes in oral protein delivery2. We have drugs cannot be given orally because they are destroyed also successfully designed pH triggered self-assembled extensively by enzymes in the gastrointestinal tract (GIT). polymers based on poly-L-lysine (PLL) for siRNA delivery In addition, the large size and water soluble nature of in cancer therapy. Using a benzoic linker which is cleaved these drugs prevent them from being absorbed through in acidic pH, we were able to attach polyethylene glycol the GIT. For siRNA based therapeutics, another challenge to (PEG) on PLL grafted with cholate hydrophobic pendant overcome is the inability of these negatively charge mol- groups. It is expected that PEG will maintain siRNA-poly- ecules to cross the cell membrane and reach its target site, mer nanocomplexes’ long circulation in the blood. How- which is the cytoplasm. We have designed a range of nov- ever, when these complexes are endocytosed by cancer el self-assembled polymers based on water soluble poly- cells, the benzoic linker will be hydrolysed in the acidic en- allylamine (PAA) for therapeutic delivery of proteins and dolysosomal compartment to detach PEG from the com- peptides. These self-assembled polymers formed nano- plexes. This will promote endosomal escape of siRNA into complexes spontaneously with model proteins such as in- the cytoplasm before it is being degraded in the endolysosome. sulin1 and calcitonin (sCT)2 with the size ranging from 100- Using a confocal microscopy, we were able to demonstrate the 250nm. The complexation took place due to electrostatic cellular uptake of these complexes by human prostate cancer and hydrophobic interaction between the polymer and cells (PC-3) and endosomal escape of siRNA, which led to in vitro proteins. As a result, the fabrication of these complexes is reporter gene knockdown. In vivo result using tumour bearing mild and unlike other conventional nanoparticles where mice showed significant tumour suppression was achieved us- the use of organic solvents and high temperature might ing VEGF siRNA-PEGylated complexes without marked toxicity degrade the labile proteins. Through grafting different and undesirable immunological response5. In conclusion, by types of hydrophobic pendant groups such as cetyl, cho- tailoring the polymer architecture, we are able to design and lesteryl and palmitoyl chains onto PAA, we were able to engineer a range of versatile nanocarriers based on self-assem- engineer different types of nano-complexes (i.e. vesicles, bled polymers which showed promising potential in the deliv- nanoparticles) with different complexation efficiencies1,3. ery of therapeutic macromolecules.

REFERENCES 1. Thompson C, et. al. International Journal of Pharmaceu- tics 383: 216-227, 2010. tics 376: 46-55, 2009. 4. Thompson C, et. al. Pharmaceutical Research, in press, 2. Cheng WP, et. al. Journal of Controlled Release 147: 289-297, 2010. 2011. 3. Thompson C, et. al. International Journal of Pharmaceu- 5. Guo J, et. al. manuscript in preparation, 2011.

International Symposium on Drug Research & Development 2011 15 DRD 2011 I-02 THE USE OF NOVEL ENABLING TECHNIQUES TO OVERCOME DRUG SOLUBILITY ISSUES Mohammed RAHMAN1, Firas EL-SALEH2,*, Tim BEE3 LECTURES 1ISP Pharma Systems LLC, Columbia, Maryland, USA 2ISP Global Technologies Deutschland GmbH, Cologne Germany 3ISP, Wayne, New Jersey, USA *[email protected] ORAL PRESENTATIONS

olubility of drugs has become a major issue in the This paper provides an overview of different excipients last few years. It has been estimated that 40–60% and techniques necessary to serve this purpose. However, Sof drugs in development have poor bioavailability the main focus is put on the technologies used in preparing due to low aqueous solubility. This trend has driven increas- solid dispersions, namely Spray Drying and Hot Melt Extru- ing interest in technologies that help increase drug solubility sion (HME). Practical considerations and the main factors in- and / or drug dissolution rate and thus move the drugs from fluencing the formation of solid dispersions supported with BCS Class 2 (good permeability, poor solubility) into BCS examples are discussed as follows: Class 1 (good permeability, good solubility), and thus overcome bioavailability issues, interpatient differences, food ef- Polymers and API miscibility fects, etc. Solubility in solvents Influence of formulation on process technology Based on the physicochemical properties of APIs, differ- Thermal behavior, instability ent formulation techniques and process technologies are Thermoreological characteristics necessary to enhance drug solubility in vivo. Process parameters and machine set-up Factors influencing physical stability

International Symposium on Drug Research & Development 2011 16 DRD 2011 LECTURES I-03 NEW TRENDS IN PHARMA: THE GROWTH OF GENERICS Farhad FARSHI Abdi İbrahim İlaç San. ve Tic. A.Ş. Sanayi Mah. Tunç Cad. No:3 Esenyurt İstanbul, Türkiye [email protected]

harma landscape is changing due to demographic, traditional business models and look for the opportunities to epidemiological and economic shifts. Growing and compensate their loss in those markets. Paging population, diseases and medical needs has been offering some huge opportunities for Pharma. The How does this new pharmaceutical environment look like? markets of the developing world are changing even more Multinational pharma companies have been challanged radically than those of the developed world. While there for variety of issues in emerging, mature and developed mar- are significant opportunities in the developing world due to kets. First, they strengthened their presence in those markets health care awareness both of governments and individuals, with acquisitions and mergers. Since 1999, 60% of the top in case of developed countries, political compulsions to re- 25 generic companies from all around the world acquired. duce health care budgets has a direct impact on profitability Second, outsourcing some of their activities to different in- of pharma sector. stitutes, companies from all around the world. It is predicted that 50% of Big Pharma R&D is outsourced to more capable The complex structure of current pharma R&D proces- firms in order to maintain a strong pipeline for future drugs. ses and studies needed to meet expectations of regulatory This will result in greater profitability and increased share- agencies have made the big pharma less productive. Big holder value for the early adopters of Big Pharma. pharma started to lose their market share, growth and profitability in the markets they are strong for many years. Drug This presentation analyses the global pharmaceuticals mar- pricing and reimbursement policies or legislations favoring ket with respect to growing generics and emerging markets. It growth of generics have a major impact on profitability of in- is also aimed to show the challanges and the opportunities for novator companies. They have been forced to change their multinational companies along with big generic players.

International Symposium on Drug Research & Development 2011 17 DRD 2011 I-04 In Silico Design of Novel and Highly Selective Monoamine Oxidase A and B Inhibitors: Evaluation of Computational and Experimental Inhibition Values LECTURES Kemal Yelekçİ Kadir Has University, Faculty of Arts and Sciences,Computational Biology and Bioinformatics Program 34083 Fatih- İstanbul, Türkiye ORAL PRESENTATIONS

onoamine oxidases are flavoenzymes bound on its binding affinity. The dispositions of the candidate mol- to the mitochondrial outer membrane. There ecules within the organism are checked by ADMET_PSA_2D Mare two isozymes named as MAO-A and MAO- (Polar Surface Area) versus ADMET_AlogP98 and their suit- B. The basic difference in these two isozymes is in their se- ability is discussed. The MAO inhibition activities of the lectivity for the oxidation of the various substrates and in- candidates are compared with the properties of selegiline hibitors. MAO-A oxidizes serotonin and norepinephrine and and moclobemide, which are the two known inhibitors of any compound selectively inhibits this isozyme possesses MAO-A and MAO-B respectively. Interaction of these can- antidepressant activity. On the other hand, dopamine is didate compounds in the active site of the isozyme will be the substrate for MAO-B and selective inhibition of MAO-B presented in detail. shows potent anti-Parkinson and plays important role in the therapy of neurodegererative disorders. That is why, they are R1 R the well known target for antidepressant, Parkinson’s dis- 4 ease and neuroprotective drugs. Recently published crystal- R3 CH lographic structures of MAO-A and MAO-B paved the way for 3 computational modeling studies. O

R5 In the present work, starting from pyrazoline scaffolds, H N N and generating thousands of structures from these, poten- R2 N tial inhibitors are obtained with their structural and physicochemical properties in order to increase both selectivity R6 S and potency toward MAO-A and MAO-B isozymes. De novo design software is used to generate the diverse structures This research was supported by The Scientific and Tech- and, three docking tools, CDOCKER, Libdock and AutoDock, nological Research Council of Turkey with a grand number are used to find the most probable potential inhibitor based 108T232.

International Symposium on Drug Research & Development 2011 18 DRD 2011 LECTURES I-05 NANOMATERIAL BASED SENSOR TECHNOLOGY FOR ELECTROCHEMICAL MONITORING DRUG-DNA INTERACTIONS Arzum ERDEM Ege University, Faculty of Pharmacy, Analytical Chemistry Department, İzmir, Türkiye [email protected]

fter the discovery of electroactivity in nucleic ac- of more-efficient gene-targeted agents3. The investigations ids1, many electrochemical approaches have been at chemistry side based on drug-DNA and protein-DNA in- Adeveloped for analyzing, or quantification of teractions would provide novel compounds to be tested nucleic acids and its interactions with drugs, toxins and pro- for an effect on a biochemical target, or would provide new teins2-12. Various type of advanced DNA biosensors have been approaches for the design of more effective DNA hybridiza- rapidly developed using different nanomaterials towards the tion biosensors based on nanomaterials, which will further goal of simple and low-cost point-of-care detection of specific become DNA microchip systems. biorecognition process using nucleic acids4, 9-12. Acknowledgements: A.E would like to express her gra- In the last decade, there has been an increasing atten- titude to the Turkish Academy of Sciences (TUBA) as the as- tion on the binding of small molecules to nucleic acids. sociate member of TUBA for their support. Such studies have a key importance for the rational design

REFERENCES 1. Palecek E. Oscillographic Polarography of Highly Polym- and indicator-free magnetic assays connected with dis- erized Deoxyribonucleic Acid. Nature 188: 656-657, 1960. posable electrochemical nucleic acid sensor system. Ta- 2. Wang J. From DNA biosensors to gene chips. Nucl. Acids lanta 78: 187-192, 2009. Res. 28: 3011-3016,2000. 9. Erdem A, Papakonstantinou P, Murphy H. Direct DNA Hy- 3. Palecek E, Fojta M. Detecting DNA hybridization and bridization at Disposable Graphite Electrodes Modified damage. Analytical Chemistry 73:74A-83A, 2001. with Carbon Nanotubes. Analytical Chemistry 78: 6656- 4. Erdem A. Nanometarial based electrochemical DNA sens- 6659, 2006. ing strategies. Talanta 74: 318-325, 2007. 10. Karadeniz H, Erdem A, Çalışkan A, Pereira CM, Pereira EM, 5. Wang J, Kawde A-K, Erdem A., Salazar M. Magnetic bead- Ribeiro JA. Electrochemical sensing of silver tags labelled based label-free electrochemical detection of DNA Hy- DNA immobilized onto disposable graphite Electrodes. bridization. Analyst 126: 2020-2024,2001. Electrochem. Commun, 9: 2167-2173, 2007. 6. Erdem A, Pividori MI, Lermo A, Bonanni A, del Vale M, 11. Erdem A, Karadeniz H, Çalışkan A. Single walled carbon Alegret S. Genomagnetic assay based on label-free elec- nanotubes modified graphite electrodes for electro- trochemical detection using magneto-composite Elec- chemical monitoring of nucleic acids and biomoleculer trodes. Sensors and Actuators B: Chem. 114: 591-598, interactions. Electroanalysis 21: 464-471, 2009. 2006. 12. Yapasan E, Çalışkan A, Karadeniz H, Erdem A. Electro- 7. Wang J, Xu D, Erdem A, Polsky R, Salazar M. Genomagnet- chemical investigation of biomolecular interactions ic electrochemical assays of DNA Hybridization. Talanta between platinum derivatives and DNA by carbon 56: 931-938, 2002. nanotubes modified sensors. Materials Science and Engi- 8. Karadeniz H, Erdem A, Kuralay F, Jelen F. Indicator-based neering B 169: 169-173, 2010

International Symposium on Drug Research & Development 2011 19 DRD 2011 I-06 NOVEL EXCIPIENTS – FROM SCRATCH TO LAUNCH Nils Wilhelm ROTTMANN BASF SE, Pharma Ingredients and Services, 67056 Ludwigshafen, Germany

LECTURES [email protected] ORAL PRESENTATIONS

he impact of excipients on modern pharmaceuti- • Screening of suitable monomers cal formulations has increased rapidly during the • Screening of suitable polymerization techniques Tpast years. Reasons for this trend in the pharma- • Optimization of copolymer composition ceutical industry are manifold: Due to numerous of patents • Optimization of polymerization process expiring in the next few years and at the same time a declin- • Scale up into pilot plant (1l to 4 m³) ing number of New Chemical Entities (NCE), life-cycle man- • Transfer into production ( > 4 m³ ). agement and re-formulation of the existing products with innovative excipients have gained a new importance. During these phases, application experts keep on testing the performance and quality of the new products, try- For the development of new drug delivery systems and ing to improve its characteristics constantly. Regulatory and the re-formulation of existing actives (API), innovative excipi- toxicology experts are involved in the projects from the very ents and novel applications are required. Since many years, beginning as well. BASF follows a strategy of developing novel and innovative performance excipients to serve the markets needs. Developing a novel excipient for innovative formulations has a similarity to the development of a new drug product. A strict time-line has to be followed, when a new project Therefore, many parties are involved in the excipient devel- is started in the development laboratories. Basically such a opment, within the raw material supplier as well as custom- development is structured in the phases: ers, universities and several authorities.

After launching a novel excipient, a lot of resources have • Market evaluation to be invested to facilitate an easy introduction and an easy • Definition of project goal registration with the new excipient.

International Symposium on Drug Research & Development 2011 20 DRD 2011 LECTURES I-07 COLLODAL CARRIERS FOR ANTICANCER DRUG DELIVERY – FORMULATION ASPECTS Marija GLAVAŠ-DODOV1, Sema ÇALIŞ2, Maja SIMONOSKA1,Nikola GESKOVSKI1, Katerina GORAČINOVA1* 1Faculty of Pharmacy, University of Sts Cyril and Methodius, Skopje, Macedonia 2Faculty of Pharmacy, University of Hacettepe, Ankara, Türkiye *[email protected]

hemotherapy has an important place in clinical The influence of different factors on the endothelial and management of cancer and the molecular com- epithelial EPR mediated uptake of the colloidal particles is Cplexities associated with the drugs as well as inac- however not fully understood. For the extravasation of the cessibility of most physiological targets have resulted with drug loaded carrier more selectively at tumor tissues, at least the development of alternative therapies as an approach some properties of the nannocarriers are particulary impor- to medical intervention (Wang et al., 2009). On one hand, tant. To successfully take advantage of NP for drug deliv- genomics and proteomics research are identifying new tu- ery, a number of significant parameters, including stability, mor-specific molecular targets, and on the other, innovative drug loading capacity, size, size distribution, zeta potential, drug-delivery systems are being designed to guide drugs surface hydrophilicity and/or hydrophobicity, and particle more precisely to tumor cells, away from sites of toxicity and decoration with specific and nonspecific ligands in order to to maintain drugs at therapeutic concentration over pro- improve cell/tissue NP interaction and internalization have longed time periods1. The overall benefit of these improve- to be carefully considered and optimized for each applica- ments in disease treatment would be an increase in patient tion. Also, introduction of in vivo biodistribution studies compliance and quality of life. Nanoparticle (NP) delivery of and in vitro cell culture internalization and efficacy experi- anticancer drugs to tumor tissue can be achieved by either ments, as early optimization tool for the design of targeted passive or active targeting. Passive targeting takes the ad- colloidal drug carriers will properly evaluate the efficacy and vantage of inherent size, physico-chemical properties of NPs potential of surface modification for active targeting and and exploits the unique anatomical and patophysiological improved drug concentration and localization at the site abnormalities of tumor vasculature, which is regarded as a of action4. Following the principles of passive and nonspe- gold standard in the design of new anticancer delivery sys- cific active targeting we have designed polyelectrolyte drug tems1-3. It is hypothesized that phenomenon equivalent to delivery systems with pH dependent swelling and muco/ EPR (enhanced permeability and retention) effect for drug bioadhesivity. In vitro cell culture studies of micro/nanopar- targeting due to increased endothelial permeability, i.e. epi- ticulated 5-FU loaded and WGA functionalized bioadhesive thelial EPR effect, might be used as potential strategy that carriers designed using principles of epithelial EPR targeting enables inflamed tissue in GI tract to be targeted. Morpho- plus nonspecific ligand functionalizatioin point to increased metric analysis of mucocellular layer overlying colorectal intracellular localization of the anticancer agent, which is cancer point that inflammatory cells are predominant in the the major component for increased anticancer efficacy of hypercellular mucocellular layer of colorectal cancer closely the drug delivery system5. In vivo biodistribution studies resembling the abundance of monocytes, macrophages, for these carriers were in favor of increased localization and dendritic cells and T cells at the site of inflamation. This concentration at the site of patophysiological abnormalities. means that epithelial EPR effect strategy and improved ac- However, the primary concerns of any targeted drug delivery cumulation of specially designed nano/microparticles at the system still stands for the abilities to successfully load and site of inflammation might be useful for targeting GI cancer deliver a desired therapeutic cargo to its target, and drug as well. loading can vary greatly with different carrier materials and fabrication methods. Appropriate drug loading goes hand-

International Symposium on Drug Research & Development 2011 21 DRD 2011

in-hand with drug release kinetics and, hence, the overall ef- might be rapid micromixing to induce faster supersatura- fectiveness of the targeted therapy. Nanoparticles formulat- tion, polymer agregation and particle formation. Also we ed using biodegradable PLGA:Poloxamer blends are among hypothesized that dispersing the drug water solution into the most intensively investigated drug delivery systems. the organic polymer solution (nonsolvent for the drug sub- Available strategies for surface modification by adsorption stance) prior nanoprecipitation, might delay the hydrophilic

LECTURES or covalent binding further increase the potential of these drug partitioning into the outer water phase during nanopri- systems for anticancer drug delivery. However, commonly cipitation. Including these principles we developed modified utilized techniques for nanoparticle preparation (emulsifi- nanoprecipitation method for Irinotechan HCl loading into cation solvent evaporation, emulsification solvent diffusion, amphiphilic PLGA nanocarriers. First Irinotechan HCl was dis- double emulsion solvent evaporation and nanoprecipitation solved in small quantity of water and dispersed in polymeric or solvent displacement) usually do not provide conditions (PLGA/amphiphillc polymers) acetone solution (ultraturax, for good encapsulation efficiency of hydrophilic anticancer 6500 rpm, Irinotechan is practically insoluble in water) which ORAL PRESENTATIONS drugs because of the rapid partitioning of the drug into the was consequently mixed in water to induce nanoprecipita- external aqueous phase. However, there are only few at- tion (ultraturax 6500 rpm). The method was highly repro-

tempts through the literature to establish modification of ducible with nanoparticle size of d(0.5) 100 nm and efficacy of nanoprecipitation method for production of hydrophilic loading ranging from 52 – 67% depending on the concen- drug loaded particles, but with even less success compared tration of Irinotecan HCl solution dispersed within polymeric to the emulsification diffusion methods. Formation of sub- acetone solution. Application of other solvents like ethanol microne particles during the nanoprecipitation method de- and acetonitrile resulted with very poor incorporation effi- pends on the differences in the surface tension between the cacy compared to water probably because of the difference solvents, which leads to interfacial turbulence resulting with in surface tension, mixing and diffusion among water (71.99 breaking up the organic phase and dispersing it as a drops mN/m) and aceton (22.73 mN/m), compared to acetonitrile in the aqueous phase6. These droplets continuously brake (28.34 mN/m) and ethanol (21.80 mN/m) (Irinotechan HCL down into smaller submicrone droplets due to the interfa- is sparingly soluble in water, ethanol and slightly in aceto- cial convective flow which contributes to renewing the in- nitrile). terfacial surface increasing the mass-exchange rate between the phases. During the diffusion of the organic solvent into Increased plasma residence time and targeting due to the water dissolved polymer chains are also dragged into endothelial EPR effect is well documented in literature, and the water medium which is followed by aggregation and was confirmed for these systems through our experiments. NP formation. In the standard procedure the organic phase Further comparative studies will be done for comparison of containing the polymer that will form the nanoparticles is localization of nanoparticles due to EPR effect and due to poured into the aqueous phase under slight magnetic stir- active targeting after attachment of specific ligand at the ring. Logical approach to improve hydrophilic drug loading nanopaticle surface.

REFERENCES 1. Acharya S, Sahoo SK. PLGA nanoparticles containing vari- model of induced colitis. J Drug Target 17 (10): 788-802, ous anticancer agents and tumour delivery by EPR effect. 2009. Adv Drug Deliv Rev doi:10.1016/j.addr.2010.10.008, 2010. 5. Glavas-Dodov M, Calis S, Simonoska-Crcarevska M, 2. Muggia FM. Doxorubicin-polymer conjugates: further Geskovski N, Petrovska V, Goracinova K. Wheat germ demonstration of the concept of enhanced permeability agglutinin-conjugated chitosan-Ca-alginate micropartic- and retention. Clin Cancer Res 5: 7–8, 1999. les for local colon delivery of 5-FU: Development and in 3. Maeda H. SMANCS and polymer-conjugated macromo- vitro characterization. Int J Pharm 381: 166-175, 2009. lecular drugs: advantages in cancer chemotherapy. Adv 6. Mora-Huertas CE, Fessi H, Elaissari A. Influence of process Drug Deliv Rev 46: 169–185, 2001. and formulation parameters on the formation of submi- 4. imonoska-Crcarevska M, Glavas-Dodov M, Petrusevska cronparticles by solvent displacement and emulsification G, Gjorgoski I, Goracinova K. Bioefficacy of budesonide diffusion methods. Critical comparison. Adv Colloid In- loaded crosslinked polyeletrolyte microparticles in rat terface Sci doi:10.1016/j.cis.2011.02.005, 2011.

International Symposium on Drug Research & Development 2011 22 DRD 2011 LECTURES I-08 NOVEL NANO-CARRIERS BASED ON SELF-ASSEMBLING POLYMERS: A NEW OPPORTUNITY FOR IMPROVING TREATMENT OF DISEASES Woei Ping CHENG School of Pharmacy, University of Hertfordshire, College Lane, Hatfield, UK AL10 9AB [email protected]

t has been estimated that 40% of the current drug enteral delivery. PAA grafted with aromatic pendant groups candidates in development and marketed drugs con- and cholestryl pendant groups enhanced the encapsulation Isist of hydrophobic drugs1. Poorly water-soluble drugs of a range of hydrophobic drugs such as etoposide, griseo- present a major challenge to the pharmaceutical industry fulvin, prednisolone, triamcinolone acetonide, propofol and as it can hinder or even prevent the progress of the drug estradiol. The drug water solubility increased from 13 to 557- into clinical use. Self-assembling polymers consisting of hy- fold depending on the type of the drug or the hydrophobic drophilic and hydrophobic segments are being explored as pendant group attached to PAA. In vivo study showed the potential drug delivery systems for hydrophobic drugs since ability of these nano-carriers in promoting oral absorption 1990s. They form different types of nano-size self-assemblies of griseofulvin in rats3. We also investigated the potential such as polymeric micelles, vesicles, nanoparticles, disc-like of these nano-carriers in pancreatic cancer therapy. Our re- structures in aqueous environment upon the aggregations sult showed that cholesteryl- PAA was able to encapsulate a of hydrophobic moieties. The hydrophobic core can be used novel hydrophobic anticancer drug and enhanced the drug to encapsulate hydrophobic drugs for improving drug solu- cytotoxic effect on human pancreatic carcinoma cells at a bility and stability. Today the most widely explored self-as- non-cytotoxic concentration. In vivo result demonstrated sembled polymer architecture is block copolymer while graft the ability of this formulation to impede tumour growth on polymer is less reported in the literature. Our work focus on xenograft mice with results comparable to gemcitabine, the the design of novel graft polymers consisting of water solu- gold standard therapy for pancreatic cancer when admin- ble polymer backbone, polyallylamine (PAA) grafted with hy- istered peritoneally4. In conclusion, nano-carriers based on drophobic pendant groups2. Generally, nano-carriers formed self-assembling polymers show promising potential in en- by self-assembling polymers are mainly investigated for in- hancing hydrophobic drug solubility and provide a new op- travenous delivery. Here, we investigate their potential as portunity to improve the treatment of diseases. hydrophobic drug solubilisers for oral, ocular as well as par- REFERENCES 1. Kilpatrick P. Nature Reviews Drug Discovery 2, 337, 2003. 3. Hoskins C, et. al. manuscript in preparation, 2011. 2. Hoskins C, et. al. Polymers for Advanced Technologies, in 4. Hoskins C, et. al. Pharmaceutical Research 27, 2694-2703, press, 2011. 2010.

International Symposium on Drug Research & Development 2011 23 DRD 2011 I-09 INSULIN THERAPY & ROUTES OF ADMINISTRATION Ercan TUNCEL Uludağ University, School of Medicine, Department of Endocrinology and Metabolism, Bursa, Türkiye LECTURES ORAL PRESENTATIONS

nsulin and insulin treatment, in general, the problems fect of parenteral insulin at cellular level is decreasing, and in of production, oscillation and the effect can be exami- particular according to the circadian rhythm can not be an Ined on the topic. adaptation. Today, the most important problem of applied insulin therapy which insülin normally reach to the liver from 1. Production the portal vein, these effects of insulin provided by giving 2. Coordination with other cells of the islet the caval system. In parenteral treatment, hepatic physiolog- 3. Oscillation dynamics ical insulin levels more than 5-10 times the amount of insulin 4. Delivery to the circulation but can pose with the effect. In other case, half life of venous 5. Impact the formation and termination of the effect insulin is around 5 minutes, the effect of treatment, subcutaneous and intramuscular applications, such as watches Forms of insulin therapy applied today, the first in the on going and life-threatening complications of hypoglyce- beta cell insulin production and stored in vesicles outside mia is important issue. New treatment methods (pancreas the cell to be synchronized with other cells is not provided. transplantation, islet replacement, intraperitoneal injection Insulin molecule in vitro conditions applied to the original pumps, subcutaneous pump systems with glucose sensor, molecule imitation by parenteral route. Pulsatile release of insulin molecule changes) is to resolve all the problems men- insulin and other hormones levels in a situation according tioned above as intense. Today, however, at this point is still to the balance of construction-oscillation. Therefore, the ef- not obtained complete success.

REFERENCES 1. Rhodes CJ, Shoelson S, Halban P. Insulin biosynthesis, patients using different simulation models. Ind Eng Chem processing and chemistry. In: Kahn RC (editor), Joslin’s Di- Res 48 (9): 4402-4414, 2009. abetes Mellitus. 14th ed. Lippincott Williams and Wilkins 4. Hanley SC, Austin E, Assouline-Thomas B, Kapeluto J, Bla- Co, Philadelphia, 2005, p. 65-82 ichman J, Moosavi M, Petropavlovskaia M, Rosenberg L. 2. Manesso E, Toffolo GM, Saisho Y, Butler AE, Matveyenko {beta}-Cell mass dynamics and islet cell plasticity in hu- AV, Cobelli C, Butler PC. Dynamics of beta-cellturnover: man type 2 diabetes. Endocrinology 151 (4): 1462-72, Evidence for beta-cell turn over and regeneration from 2010. sources of beta-cells other than beta-cell replication in 5. Monte SV, Schentag JJ, Adelman MH, Paladino JA. Glu- the HIP rat. Am J Physiol Endocrinol Metab 297 (2): 323- cose supply and insulin demand dynamics of antidiabetic 30, 2009. agents. J Diabetes Sci Technol 4 (2): 365-81, 2010. 3. Farmer TG, Edgar TF, Peppas NA. Effectiveness of intravenous infusion algorithms for glucose control in diabetic

International Symposium on Drug Research & Development 2011 24 DRD 2011 LECTURES I-10 ORAL ANTIDIABETIC DRUGS Nilgün Güvener DEMİRAĞ Başkent University, Department of Internal Medicine, Divison of Endocrinology and Metabolism, Ankara, Türkiye [email protected]

he incidence of type 2 diabetes is epidemically in- Although the large number of therapeutic choices now creasing worldwide. Developments of appropriate available, it has been shown that HbA1c level still above 7% Tstrategies to prevent and to treat the diabetes be- for many diabetic patients. Oral antidiabetic therapy is the come more important and challenging. Main goal of our treat- main treatment of choice for diabetic patients regardless of ment is to have the best glycemic control. While achieving this duration of disease, metabolic control, complications and goal, side effects, weight changes, hypoglycemic symptoms presence of cardiovascular risk factors and intensification of should be in acceptable range. In addition to these, we also treatment is usually not good enough. expect these drugs to reserve or even increase the pancreatic b cell functions and provide advantages such as prevention Type 2 diabetes is a progressive disease therefore; preser- or control of hypertension, hyperlipidemia, cardiovascular dis- vation of b cell function must be the one of the main treat- eases which are commonly seen in diabetics and should be ment goals while developing new treatment strategies. As cost effective. Characteristics of currently used antidiabetic we understand the pathogenesis of diabetes, we would be medications are summarized in the table below. able to develop new treatment goals and alternatives.

Interventions Expected decrease in HbA1c Advantages Disadvantages

Lifestyle 1-2 Low cost, many benefits Most patients fail within 1 year modifications

Weight neutral, Metformin 1-1.5 GI distress, lactic acidosis inexpensive Hypoglycemia, weight gain, insufficient effect on Sulfonylureas 0.8-1.5 Inexpensive preservation of β cell function, adverse effects on ischemic remodelling? Weight gain, edema, anemia, Thiazolidinediones 0.8-1.0 Improved lipid profile osteoporosis, possible CV risks, (glitazones) expensive GI side effects, injection, GLP-1 analogs 0.8-1.2 Weight loss expensive No need for dose Expensive, short duration of DPP-4 inhibitors 0.5-0.9 adjustment, high experience tolerability, weight neutral Alpha-glucosidase Frequent GI side effects, three- 0.5-0.8 Weight neutral inhibitors times daily dosing

International Symposium on Drug Research & Development 2011 25 DRD 2011 I-11 NEW ANTIDIABETIC AGENTS Bülent Okan YILDIZ Hacettepe University, School of Medicine, Department of Internal Medicine,

LECTURES Endocrinology and Metabolism Unit, 06100 Sıhhiye, Ankara, Türkiye ORAL PRESENTATIONS

ncreasing realization of the need for optimal glycemic past decade, increased understanding of the broader patho- control and the shortcomings of available therapeutic physiology of type 2 diabetes has led to the development Ioptions in diabetes have led to active search for new- of new agents. Incretin-based therapies represent one such er and improved therapeutic modalities. Physicians have group of drugs in the pharmacotherapy of diabetes. Several high expectations for the efficacy and safety of new drugs. novel classes of drugs with different mechanism of action are New antidiabetic agents should offer clear advantages over under development. Potential molecular targets in adipose available agents, lowering glucose via mechanisms ideally tissue and kidney receive particular attention. associated with beneficial cardiovascular effects. Over the

International Symposium on Drug Research & Development 2011 26 DRD 2011 LECTURES I-12 TO OVERCOME THE FEAR OF JOB INTERVIEW: APPROACHES WITH SOCIAL EFFECTIVENESS AND DIALECTICAL BEHAVIOR Nesrin DİLBAZ Ankara Numune Research and Training Hospital, Türkiye

reparing for job interview can be stresful. The fear level goes up and make a peak and takes more time to return of negative evaluation can be basic emotion dur- base. This is why some people are experiencing more crises Ping interview. The ways to overcome fear during than others. They dont have enough methods for coping job interview, To avoid nervousness during interview, How with these emotions. DBT is a method for teaching coping to feel prepared for job interview are the most frequent pro- and social effectiveness that will be helpful for improving the grams that are prepared for succesful interview. lifes of these individuals.

Dialectical Behavior Therapy (DBT) is built by modifying The aim of this presentation is teaching individuals to components of Cognitive Behavior Therapy and adding Zen cope with negative evaluation anxiety and fear and also and mindfullness. According to DBT some people react ab- training them about social effectiveness and social skills that normally to emotional stimulation due to environments dur- will help these individuals to improve their lives. ing upbringing and due to biological factors. Their arousal

REFERENCES 1. McKay et al. Dialectical Behavior Therapy Skills Work- 2. Samuel MT, Deborah CB, Michele RC. Social effectiveness book: Practical DBT Exercises for Learning Mindfulness, therapy: A program for overcoming social anxiety and so- Interpersonal Effectiveness, Emotion Regulation, & Dis- cial phobia: A therapist guide (1997). tress Tolerance (2007). 3. Blonna R. Maximize Your Coaching Effectiveness with Ac- ceptance and Commitment Therapy (2011).

International Symposium on Drug Research & Development 2011 27 DRD 2011 I-13 PERSONAL BEHAVIORS DURING JOB INTERVIEW Aykut BORA Bilim Pharmaceutical Company, Türkiye LECTURES ORAL PRESENTATIONS

he range of tasks in a pharmaceutical company and retaining the competencies the company needs in order spans a wide area of different job descriptions and to realise its future goals. Texpert knowledge, from the development of medicines to their production, the application for the necessary Our competency management process comprises the ac- permits, their marketing and communication, to the evalu- tivities of recruitment of candidates with the defined skill and ation and reporting on the effects of new pharmaceuticals. qualifications, of monitoring their performances, of personal development, motivation and retention in the company. When a new product is defined a team needs to be established to design it and a process for its cost-efficient With the various practical implementations at our com- manufacture for a large customer group. When setting up pany, we pursue the objective of developing the skills of new such teams, successful and leading companies that are the team members and of our present staff. With this approach preferred choice of employees also successfully apply com- we support in particular university students with an inter- petency management. At Bilim İlaç one of our HR priorities est in our trainee programme. Every year, our company ac- is competency management. Our competency management cepts trainees from different university departments. Once process, which has been designed in line with our company’s we have reached the employment stage, those among them strategies and objectives, is based not only on the principle who stand out in terms of performance and potential are of identifying the best employees and leadership personnel subject to our selection and recruitment process which en- of the future, but also on the principles of defining, acquiring sures that their current potential is fully appreciated.

International Symposium on Drug Research & Development 2011 28 DRD 2011 LECTURES I-14 ABOUT THE REQUIREMENTS OF SCIENTIFIC BACKGROUND FOR JOB APPLICATION IN DRUG RESEARCH AND DEVELOPMENT A. Atilla HINCAL Dean of Hacettepe University Faculty of Pharmacy (1981-94); Head of Institute of Health Sciences (1994-97) İDE Drug Information Consultancy and Education Ltd. Co., Ankara, Türkiye İDE Pharmaceutical Consultancy Ltd. Co., Kavaklıdere, Ankara, Türkiye [email protected], [email protected]

bviously, educational background is among top well positioned to accurately weigh their own potential for factors that impact on how successfully a candi- success in a given field. It should be never overlooked that Odate can perform at an R&D position. However, wanting something and achieving it successfully are not the several other parameters also factor in, including work per- same thing. A person’s success is proportional to the degree formance, attitudes, image, achievements and efficiency of by which such person is able to accurately identify the areas the candidate in the school and thereafter, if applicable, in and issues in which he or she will be able to perform research the workplace, albeit short. An indispensable point that must tasks or any other job as best as he or she can, while loving it not be overlooked is the quality of the education received, dearly and when circumstances warrant it, by making a sacri- and whether the person in question will be able to apply his fice. And for persons intending to pursue a career in R&D, this or her attributes in the most appropriate and effective way to means performing a seriously thorough and down-to-earth perform in a manner that will best respond to the expecta- analysis of both themselves and of the job they are seek- tions of both himself and the company/establishment that ing to get, weighing it physically, mentally, and financially intends to employ him or her. to decide whether they are in fact up to it. They must know that scientific research and development is a marathon of an What we all know, or should now, that at the end of the undertaking that requires sacrifice, constantly working, ob- day the success and the returns on such success belongs serving, performing new analyses and syntheses using all of primarily to the individual. In fact, achievements of success- these inputs, while building and showcasing a creative side. ful individuals that a county is able to generate are a major Scientific methodology requires a knowledge of past work driver of growth and development for countries. A candidate in the field and of comparables before embarking on a re- to a position should therefore carefully weigh whether he or search undertaking in a specific field. Nevertheless, it must she is possessing the necessary competencies; more so in be understood, absorbed, acknowledged and never forgot- pharmaceutical R&D, which is highly versatile and where it ten that science cannot be constructed on replicates, errors, carries much more relevance. Main expectations from those and false findings. who intend to get into R&D include the ability to instill trust in others, and possessing the essential characteristics of a What do we do, think, want to do, can do and what should person of science. And for newcomers this means not letting be look out for in this speech, when applying for a job/a the years in school go to waste, and learning, and under- position at a science institute, in the school, during youth, standing that learning is the most important gain and that mid-life and maturity? Had it been possible to know all of success, not only in sciences but in every aspect of life, will these before applying for a job, surely we would be living in come only if learnings can be put to appropriate use, and in a vastly different world than what we have now. And what the benefit of society. have we done, what are we doing, and what will we do to learn of these? We will address these issues using examples Persons considering getting into R&D should, before from actual events and experiences. anything else, know themselves very well. They should be

International Symposium on Drug Research & Development 2011 29 DRD 2011 I-15 HOW TO CHANGE AN ENZYME INTO A CYTOTOXIC AGENT: MECHANISMS OF TARGETING TOP2 IN CANCER John L. NITISS*, Anna ROGOJINA, Karthik SHANMUGANATHAM, Karin C. NITISS LECTURES Molecular Pharmacology Department, St. Jude Children’s Research Hospital, Memphis, TN 38105 USA *[email protected] ORAL PRESENTATIONS

NA topoisomerases are ubiquitous enzymes that Since topoisomerase II poisons kill cells by the gen- are required for replication, transcription, and eration of DNA damage, we hypothesized that under- Dmany other chromosomal processes1. DNA topoi- standing mechanisms for repairing or tolerating this somerases make transient breaks in DNA using a unique type of enzyme mediated DNA damage would increase mechanism that includes the creation of a transient enzyme/ our ability to predict which tumors might be sensitive DNA covalent intermediate. Many small molecules target- to topoisomerase poisons, and to design safer rational ing these enzymes have been identified that exploit this combinations of topoisomerase poison with other anti- enzymatic mechanism and increase the level of enzyme co- cancer drugs. We were particularly interested in genes valently bound to DNA. The generation of elevated levels of that were important for repair of protein/DNA adducts, enzyme/DNA covalent complexes is the key event in cell kill- Therefore, we concentrated on proteins that may be in- ing by drugs targeting DNA topoisomerases, and agents that volved in nucleolytic repair of this unique adduct. We enhance levels of topoisomerase/DNA covalent complexes demonstrated that yeast and human Tdp1 could hydro- are termed topoisomerase poisons. Topoisomerase poisons lyze 5’ as well as 3’ phosphotyrosyl linkages, and play are important anti-cancer drugs, and include the camptoth- a functional role in repairing topoisomerase II medi- ecins (targeting topoisomerase I) and agents such as etopo- ated DNA damage4. Genetic and biochemical analysis side and doxorubicin (targeting topoisomerase II)2. While of the MRN complex (Mre11/Rad50/Nbs1) implicated topoisomerase poisons are active anti-cancer drugs, there this protein in the removal of the topoisomerase–like are only limited tools available to predict which patients will protein Spo11 from the ends of DNA during meiotic re- respond to this class of agents. combination. The Mre11 protein carries both endonu- clease and exonuclease activities. We used an assay for Most topoisomerase poisons are a class of inhibitors quantitating topoisomerase II/DNA covalent complex- termed interstitial inhibitors3. This mode of inhibition es in mammalian cells, and showed that in the absence depends on both the enzyme and DNA to form a drug of the MRN complex, levels of topoisomerase II/DNA binding site. There is limited information about how covalent complexes were substantially elevated. These topoisomerase II and DNA combine to form a drug results show at least two pathways that are involved in binding site for agents such as etoposide and doxoru- nucleolytic repair of topoisomerase II mediated DNA bicin. We have combined genetic and structural ap- damage. Our studies with Tdp1 and the MRN complex proaches to identify regions of topoisomerase II that provide a strong validation for the use of genome wide are important for drug action. We identified sites near screens in model organisms to study anti-cancer drug the active site tyrosine that contribute to drug sensitiv- action, coupled with the development of specific bio- ity. Interestingly, we also identified a domain near the chemical assays that can be used to functionally assess C-terminal dimerization domain that also controls DNA the importance of specific proteins in drug effects. cleavage. This result suggests that it may be possible to identify potent allosteric inhibitors of topoisomerase II that may have unique therapeutic potential.

International Symposium on Drug Research & Development 2011 30 DRD 2011 LECTURES REFERENCES 1. Nitiss JL. DNA topoisomerase II and its growing reper- 3. Pommier Y, Cherfils J. Interfacial inhibition of macromo- toire of biological functions.DNA topoisomerase II and its lecular interactions: nature’s paradigm for drug discovery. growing repertoire of biological functions. Nat Rev Can- Trends in Pharmacological Sciences 26: 138-145, 2005. cer 9: 327-337, 2009. 4. Nitiss KC, Malik M, He X, White SW, Nitiss JL. Tyrosyl-DNA 2. Nitiss JL. Targeting DNA topoisomerase II in cancer che- phosphodiesterase (Tdp1) participates in the repair of motherapy. Nat Rev Cancer 9: 338-350, 2009. Top2-mediated DNA damage. Proc Natl Acad Sci USA 103: 8953-8958, 2006.

International Symposium on Drug Research & Development 2011 31 DRD 2011 I-16 ENHANCED SURVIVAL AND PARACRINE ACTIVITY OF BONE MARROW MESENCHIMAL STEM CELLS: IMPACT ON CELL THERAPY OF ISCHEMIC SYNDROMES LECTURES Angelo PARINI1,*, Céline MIAS1, Chiara ALFARANO1, Philippe BOURIN2, Jérôme RONCALLI1, Daniel CUSSAC1 1Inserm UMR U 1048 – Institute of Metabolic and Cardiovascular Diseases Toulouse 2Laboratoire de Thérapie Cellulaire EFS, Pyrénées-Méditerranée, Toulouse *[email protected] ORAL PRESENTATIONS

everal studies have shown that Bone Marrow Mes- drogen peroxide-dependent apoptosis. Using rat models of enchymal Stem Cells (BMMSCs) administration ischemic heart or renal failure, we showed that melatonin Senhances structural and functional recovery of in- pretreatment in vitro strongly increased survival of BMMSCs jured organs. The beneficial effects of injected BMMSCs have after intraparenchymal injection. This effect was concomitant been related, in part, to their transdifferentiation in the cell to increased angiogenesis, decreased fibrosis and improved phenotype of host organs. More recently, it has been sug- recovery of cardiac and renal functions. In order to deter- gested that BMMSCs improve tissue regeneration through mine whether the effects observed in vivo where related to secretion of a variety of paracrine factors. Approaches to im- the secretion of paracrine factors, we tested conditioned prove the ability of grafted BMMSCs to survive and secrete culture media from melatonin-treated MSCs on endothe- paracrine factors represent one of the challenges for the lial progenitor cells and fibroblasts. Our results showed that further development of these novel therapies. In our labora- conditioned media from melatonin-treated MSCs stimulate tory, we designed a strategy of ex-vivo pretreatment with the tube formation by endothelial progenitor cells and decrease pineal hormone melatonin to improve survival, paracrine ac- extracellular matrix accumulation by fibroblasts. tivity and efficiency of BMMSCs. In conclusion, our results show that melatonin behaves Experiments in vitro showed that, through stimulation as a preconditioning agent increasing survival, paracrine ac- of specific MT receptors, melatonin induced an overexpres- tivity and efficiency of BMMSCs. The use of this molecule for sion of the antioxidant enzyme catalase and superoxyde pretreatment of BMMSCs may represent a novel and safe ap- dismutase-1 and increased the resistance of BMMSCs to hy- proach for improving the beneficial effects of cell therapy of solid organs.

International Symposium on Drug Research & Development 2011 32 DRD 2011 LECTURES I-17 Serotonergic Control of Cardiovascular Function Nathalie Pizzinat Institute of Metabolic and Cardiovascular Diseases (I2MC), INSERM, Toulouse, France

erotonin, or 5-hydroxytryptamine (5-HT), is a nature. The same observation has been made in rat submitted urally-occurring vasoactive substance synthetised to cardiac hypertrophy by pressure overload suggesting a Sfrom L-tryptophan, primarily by central and periph- targeted effect of serotonin during cardiovascular patholo- eral monoaminergic neurons and the gastro -enterochro- gies. In order to address the question of serotonin function maffin cells. Serotonin released from gastrointestinal tract is during pathological heart remodeling, we used KO mice for avidly taken up and stored by circulating platelets. The car- the limiting enzyme of serotonin biosynthesis (tryptophan diovascular system is mostly exposed to free serotonin, the hydroxylase 1) TPH1. This enzyme converts L-Tryptophan to level of which is largely controlled by platelets. 5-hydroxy-L-tryptophan (5-HTP) which is then transformed into 5HT by the L-aromatic amino acid decarboxylase (LAAD). Numerous studies have demonstrated the implication of The KO TPH1 mice exhibited low level of circulating and car- serotoninnergic receptors in the control of vascular tone and diac serotonin. We submitted KO TPH1 mice and their WT lit- cardiac function. Serotonin produces complex responses on termates to a mild transverse aortic constriction (TAC). Echo- blood pressure including vasoconstrictive and vasodilatory ef- cardiographic analysis revealed in banded KO compared to fects. The vasopressor response is a consequence of vasocon- WT mice an exacerbated left ventricular dilatation and a de- striction mainly mediated by 5-HT2a receptors located on vas- crease in fractional shortening indicating a decompensated cular smooth muscle cells. The vasodepressor response may cardiac function. In this model of pressure overload hyper- involve different mechanisms: vasodilatation by endothelium trophy induced by TAC, it appears that low level of serotonin release of nitric oxide and inhibition of the vasopressor sym- worsen progression to cardiac failure. pathetic outflow by sympatho-inhibitory 5HT1 receptors. To further investigate this hypothesis, we restored 5HT Serotonin regulates cardiac function by inducing chro- level in KO TPH1 mice by supplementation with the sero- notropic and inotropic effects mediated by 5HT4 or 5HT2A tonin precursor 5-HTP. Preliminary analysis have shown that receptors. This ventricular positive inotropic responsiveness treatment with 5-HTP induced a significant decrease in ven- to serotonin exacerbates in conditions of heart failure both tricular dilatation without affecting hypertrophy, measured in rat and human ventricles. We have also underlined the by echocardiography. Moreover fibrosis was decreased in relevance of platelet derived serotonin on cardiac fibroblast ventricle indicating a beneficial effect of 5-HTP treatment. phenotype. Serotonin released by platelets, occuring princi- Fractional shortening was fully preserved in the KO TPH1 pally during thrombotic events, promotes cardiac fibroblast mice treated group. These data indicate that in vivo, normal activation through stimulation of 5-HT2A receptors. These serotonin concentrations are required to prevent transition effects of platelet derived serotonin may have particular rel- from hypertrophy to heart failure. evance in acute events following ischemic injury and in the early ventricular remodeling. These findings underline the role of serotonin in regulation of cardiovascular function and offer new prospects for Recently, an up regulation of circulating serotonin has the use of serotoninergic drugs in therapies for cardiovascu- been described in patients with cardiopathy and heart fail- lar diseases.

International Symposium on Drug Research & Development 2011 33 DRD 2011 I-18 BISACYLAZIDES: A NEW MILESTONE FOR THE SYNTHESIS OF VARIOUS HETEROCYCLES Metin BALCI LECTURES Department of Chemistry, Middle East Technical University, 06531 Ankara, Türkiye [email protected] ORAL PRESENTATIONS

socoumarins, indoles, benzoazepines represent an im- The azide derived from the half ester 3 was synthesized. portant class of naturally occurring compounds that Conversion of the formed azide into the corresponding ure- Idisplay a wide range of biological activities. Our inves- thane in methanol followed by cyclization and acetylation tigation began with an attempted synthesis of the diazide gave the indol derivative4. On the other hand, the reaction derived from the homophthalic acid1. Homophthalic acid 1 of homophthalic anhydride with hydrazine in dimethyl for- was reacted with thionyl chloride, dimethy formamide and mamide resulted in the formation of a new pyrazole deriva- sodium azide in the presence of tetrabutyl ammonium bro- tive5. mide as a catalyst. Only, 6H-dibenzo[c,h]chromen-6-one (2) O O O R O R O was formed in 41% yield 1,2. N N O NH NR NH N C N NR O O O O O O COOH COOH SOCl2, DMF O Furthermore, the synthesis of benzodiazepinone and Bu4NBr, NaN3 3 dihydrofuropyrimidinone3, isoquinolinone and furopyrrol COOCH3 1 COOH 2 starting from the corresponding diacids will be discussed4-7.

COOMe O N OH O

O N 4 NH H3C 5

REFERENCES 1. Özcan S, Şahin E, Balcı M. The synthesis of unusual isoco- 4. Dengiz Ç, Özcan S, Şahin E, Balcı M. A new synthetic umarin derivatives: the chemistry of homophthalic acid. Methodology for the construction of 1,3,4,5-tetrahydro- Tetrahedron Lett 48: 2151-2154, 2007. 2H-1,3-benzodiazepin-2-one skeleton. Synthesis: 1365- 2. Özcan S, Balci M. The Chemistry of Homophthalic Acid: 1370, 2010. A New Synthetic Strategy for Construction of Substitut- 5. Deliömeroglu MK, Özcan S, Balci M. A short and efficient ed Isocoumarine and Indole Skeletons. Tetrahedron 64: construction of the dibenzo[c,h]chromen-6-one skel- 5531-5540, 2008. etone. Arkivoc 148-160, 2010. 3. Koza G, Özcan S, Şahin E, Balci M. Regioselective Synthe- 6. Koza G, Karahan E, Balci M. Helv Chim Acta 93: 1698-1704, sis of Dihydrofuro[3,2-d]pyrimidin-2(1H)-one Skeleton: 2010. A New Class of Compounds. Tetrahedron 65: 5973-5976, 7. Özcan S, Çağatay D, Deliömeroğlu KM, Şahin E, Balci M. 2009. A novel one-pot three component reaction: Synthesis of isocoumarin-condensed pyrazols. Tetrahedron Lett 52: 1495-1497, 2011.

International Symposium on Drug Research & Development 2011 34 DRD 2011 LECTURES I-19 Dendrimers as potential drug carriers; MICROWAVE-ASSISTED SYNTHESIS OF PAMAM TYPE DENDRIMERS Cemil DIZMAN1, Tezcan PARALI1, Ali Serol ERTÜRK1, Metin TÜLÜ1,2,* 1Department of Chemistry, Fatih University, 34500 İstanbul, Türkiye 2Department of Chemistry, Yıldız Technical University, 34210 İstanbul, Türkiye *[email protected], [email protected]

oly(amido amine) (PAMAM) type dendritic of molecular electronics. With their synthetic control, macromolecules have become significant im- appearently unlimited modifications and wide variety Ppact in the field of material sciences and are of potential applications, as well as their commercial4,5 one of the major starting points for nanotechnology availability, these 1à 2 or 1à 3 branched dendrimers as a result of the numerous modifications that can be have become an important nanostructured tools for conducted, either on the surface or within their mo- diverse pratical applications. Present study6 mainly co- lecular infrastructure, thus taking advantage of their vers 1 à 3 branched non-chiral dendrimers prepared by unimolecular micelle properties1. These host cavities, a divergent process but selected functional surfaces maintained by the dendritic branches, allow for the in- having antibacterial or antimicrobial properties. As a corporation of nanoparticles as well as metal particles, synthetic method Microwave Assisted Technique has which make these attractive in catalysis and imaging been applied. More detailed; ethylenetriamine (ETA) or studies. Especially Dendritic hosts with hydrogen bon- trimethylolpropane tris[poly(propylene glycol), amine ding receptors have been made by Newkome et al.2 terminated] ether were selected as cores and methy- The poly(amidoether) dendrimers contain (2,6-diacyla- acrylate (MA) and ethylenediamine (EDA) were alterna- mino)pyridine moieties that serve as donor-acceptor- tively used as building blocks. Novel PAMAM type den- donor (DAD) H-bonding units. Barbituric acid, a guest drimers were synthesized up to the 4th. generations. that contains two ADA arrays, is bound to the dendri- In order to make the molecules water soluble, surface mer, as evidenced by 1H NMR measurements. For the groups were modified by 2-amino-2-(hydroxymethyl) higher generation dendrimers, intramolecular self- propane-1, 3-diol (AT). The syntheses were carried out association competes with guest binding. The solubility mostly by applying microwave irradiation technique of these fractal constructs can be tailored depending and correlated with conventional methods. The prod- on their surface modifications. Highly water-soluble, ucts were characterized via Elementary Analysis (EA), neutral dendrimers appended with, grown from, or ac- Fourier Transform Infra Red (FT-IR) and 1H NMR-13C NMR ting as hosts to specific molecules give rise to a wide spectroscopy. Since all dendrimer/substrate complexes variety of biomedical applications such as drug deli- were completely miscible with water in all proportions. very systems and MRI imaging agent3. The inherent When the bound substrates are drug moieties, then the supramolecular or supramacromolecular chemistry has resulting complexes could be considered as potential been exploited but the design and construction of uni- drug delivery systems. In the similiar studies (Scheme quely tailored macrostructures have just begun. Laser 1),7 flow calorimetry demonstrates that dendrimers dyes, as well as electron and energy donor and accep- were able to release their hydrophobic guests when in tor functionality, have also been paired with these frac- contact with a biological cell. tal constructs in order to probe their uses in the field

International Symposium on Drug Research & Development 2011 35 DRD 2011

HO OH OHOH HO OH OHOH HO OH HO OH HN NH HN NH HO O O OH HO O O OH HO OH HO OH NH HN NH HN HO N N OH HO N N OH O O O O O OH NH HN NH HN O O O O HO HO N OH N OH LECTURES HO HO OH O OH O O O - O HO N OH O NH OH HO N - O O NH OH N O N H O O H O O H N N H H N N H HO N N N N OH HO N N N N OH N N N N H H OH H H OH HO O O HO O O HO OH HO OH HN O O NH HN O O NH

N N N N O O O O NH O O HN OH NH O O HN OH HO HN NH HO HN NH OH OH HOHO OH HOHO OH ORAL PRESENTATIONS HO OH HO OH HO OH HO OH HO HO HO HO

A B Scheme 1. Possible interactions: Unlikely hydrogen

REFERENCES 1. Yang H, Lopina ST. Penicillin V-conjugated PEG-PAMAM 4. http://www.dendritech.com/ star polymers. J Biomater Sci Polymer Edn 14(10), 1043– 5. http://www.frontiersci.com/ 1056, 2003. 6. Tulu M, Aghatabay NM, Senel M, Dızman C, Paralı T, Dül- 2. Newkome GR, Woosley BD, He E, Moorefield CN, Guther ger B. Synthesis, characterization and antimicrobial activ- R, Baker GR, Escamilla GH, Merril J, Luftmann H. Cascade ity of water soluble dendritic macromolecules, European Polymers: Synthesis and characterization of one direc- Journal of Medicinal Chemistry 44, 1093-1099, 2009. tional arborols based on adamantane. Chem Commun 7. Beezer AE, King ASH, Martin IK, Mitchel JC, Twyman LJ, 2737-2738, 1996. Wain CF. Dendrimers as potential drug carriers; encap- 3. Newkome GR, Shreiner CD. Poly(amidoamine), polypro- sulation of acidic hydrophobes within water soluble pylenimine, and related dendrimers and dendrons pos- PAMAM derivatives. Tetrahedron 59, 3873-3880, 2003. sessing different 1 à2 branching motifs: An overview of the divergent procedures. Polymer 49, 1-173, 2008.

International Symposium on Drug Research & Development 2011 36

ORAL PRESENTATIONS

ORAL PRESENTATIONS - -

live

particle

1,2 viral

trafficking

irchhausen single

K by

Tomas , Tomas 1 endosomal entry routes by drugs such as amiloride and dynasore in or der to repress macropinocytosis or clathrin-mediated endo entered virions that indicate results Our respectively. cytosis, non-polarized cells very inefficiently both by clathrin-mediated endocytosis and by macropinocytosis-like mechanism. In contrast, efficient entry of virions at the apical surface of polarized cells was strictly mediated by clathrin-mediated endocytosis. Our data provide the first real-time analysis of virus entry into polarized cells and define the entry mechanism of reovirus. More generally, our observations empha- size the importance of studying virus entry in relevant cell types, especially for pathogens that invade hosts through epithelium. the polarized

cells

- - - 41 O-01 ulant DRD 2011 DRD and B

tracking Steeve , Steeve 1 entry

polarized

ural K and

Immune Disease Institute, Harvard Medical School, Boston, MA. School, Boston, Medical Harvard Immune Disease Institute, Department of Cell Biology, Harvard Medical School, Boston, MA. Boston, School, Medical Harvard Biology, Department of Cell 1 2 eovirus International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International R Cömert

polarized ncolytic ncolytic viruses infect and kill cancer cells - pref erentially; either by direct lysis of the tumour cells or by serving vectors for delivery of genes -

onitoring

non O M posed as a possible tumor-killing therapy for cancer treat generation ment. of However, tumour selectivity is a critical factor for constraining the oncolytic activity to cancerous employed we Here tissue. healthy the affecting without cells high-resolution fluorescence microscopy to study nalization and trafficking inter of reovirus particles in polarized epithelium and non-polarized cells. We controlled the viral encoding encoding enzymes that convert non-toxic pro-drugs into cytotoxins, e.g., ganciclovir. Recently, reoviridae family virions have been shown to have oncolytic properties and pro ORAL PRESENTATIONS conversion of 3rd conformation of conformation 3rd of conversion these types ofcompounds.these types to get in depth information about interconversion barriers of results are and unexpected more investigations are required of conformation corresponding for kcal/mol, 7.48 of 4,5- of enantiomer (S) and (R) of structures Starting calculated. version barrier,version transition state (Figure 2). The minimum calculated intercon- zero-point and thermal corrections, of the minimum and the the including energies, total the between difference the by calculated was barrier interconversion The frequency. nary imagi- one by characterized were Transitionstructures state followedcalculations.calculation IRC byfrequency a byized character was found point stationary each and optimized, state structure and the transition state geometries were fully calculations.ground The further for selected were analogue each of 1) (Figure conformations unique four optimization, After optimization. B3LYP/6-31G(d) by followed MMFF94s field force the using annealing simulated Sybyl by obtained were compound each of conformations Ten package. ing epin of C I 1S omputational dimethyl 2 -2- Department ofChemistry, Federal Urdu University ofArts,Science andTechnology, Gulshan-e-IqbalScience tions of tions conforma - different between barriers nterconversion tetrahydro 4,5- whereas the maximum interconversion barrier,interconversion maximum the whereas one 1 Institute ofChemistry, Karl Franzens University, Graz, Heinrichstrasse 28,A-8010Graz, Austria, were created with the Sybyl molecular model- molecular Sybyl the with created were dimethyl R -1,3,4,5- DG S and ≠ = -2H-1,5- 1.77 kcal/mol, was observed for inter for observed was kcal/mol, 1.77 enantiomer of enantiomer tetrahydro International Symposium onDrugResearch &Development 2011 benzodiazepin

-1,3,4,5- study Sajid 1S -2H-1,5- 4,5- to 4th conformation 4th to dimethyl Jahangir

of Campus, Karachi, Sindh,Pakistan tetrahydro benzodiaz -2-

one the *[email protected] . These 1R. -1,3,4,5-

DG DRD 2011 were

1,2,* conformational O-02 ≠ - = 42 ,Walter M.F. - - -2H-1,5- F abian benzodiazepin 1

Figure 1 Figure 2 interconversion -2- one

ORAL PRESENTATIONS - , q - acetoni in ) 4 hali K , Obaid N. indicum Extract, Glucose) have ersiani Qadri V , M. Samiuddin

trile at 100mV scan rate, where Glassy Carbon (GC) where used was trile 100mV at scan rate, the samples natural of workingInas presence the electrode. oxidation peaks of superoxide were obtained in decreased The decreased or anodic diminished current. peak oxidation current is a clear indication of antioxidant activity studied samples. Out of eleven sample, eight samples - (Gins of the ing, Turmeric, Orange juice, Almond, Pistachio, Tea, Green Tea, Olive oil) have shown high antioxidant activity where as three sample (Vinegar, activity. antioxidant low shown Superoxide Superoxide free radical was generated by the run of CV of (TBAClO perchlorate tetrabutylammonium 0.1M Mohammad Ali Mohammad , , - 43 atif O-03 L DRD 2011 DRD ahiri T , M. *[email protected] Karachi-75300, Pakistan Pakistan Karachi-75300, assan H Fahad Fahad Iftikhar Ahmad , Iftikhar * International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International uhammad IMPORTANT SAMPLES THROUGH CYCLIC VOLTAMMETRY

M raditional herb medicines are an importantan partare herbmedicines raditional of the health care system of Subcontinent of South Asia. Ayurveda, supposed to be the oldest medi-

Narrium indicum Extract, Glucose) were selected to Haji Department of Chemistry, Federal Urdu University of Arts, Science and Technology, Gulshan-e-Iqbal Campus, and Technology, of Arts, Science University Urdu Federal Department of Chemistry,

DETERMINATION OF ANTIOXIDANT ACTIVITY OF SOME BIOLOGICALLY T cal system in the world, provides potential leads to find ac tive tive and therapeutically useful compounds from plants. In the present work eleven natural samples (Turmeric, Orange juice, Almond, Pistachio, Tea, Ginsing, Green Tea, Olive oil, Vinegar, explore their antioxidant activities through cyclic - voltam metry (CV). Although most of them are already known for their antioxidant activities but this is the first time that their antioxidant properties have been investigated through CV. ORAL PRESENTATIONS ity control tests, control ity qual- the After 4. and 3 between pH of adjusting performed was technetium-99m with FOL-PEG-DOX SEM5. of Radiolabelling and zetasizer spectroscopy, NMR by characterized was nanoconjugate this and study as previous a in described prepared was conjugate (FOL-PEG-DOX) doxorubicin glycol)- Folate-poly(ethylene targeting. for agent imaging cancer a as potential radiopharmaceutical its into research and technetium-99m with labelling conjugate, doxorubicin folate-PEG- of synthesis is work this of aim The 4. side-effect severe dose-limiting a is erythrodysesthesia plantar palmar of toxicities, the most important is the cardiotoxicity, but also and the clinical use of doxorubicin shows a large-spread ﬁeld action antineoplastic of spectrum broad a has doxorubicin antibiotic anthracycline The tissue3. cancer to agents aging im- and drugs cytotoxic of targeting the in use for teristics etc.)2. Thereforecharacdesirabledisplays folicmultiple acid nanoparticles, liposomes, proteins,agents, imaging peutics, acid and folate-linked cargos of many sorts (i.e., chemothera- folic both transport to ability the has FR brain. and throat, nose, prostate, lung, colon, gland, mammary ovary, the of cancers epithelial on overexpressed are FRs example, For cells.cancer on numbers large in present often are but cells, studies on male rats and the animal experiments were ap were experiments animal the and rats male on studies ( 99m P Tc-PEG-DOXand RADIOLABELLING WITH TECHNETIUM-99 WITH RADIOLABELLING ceptors (FR) exhibit limited expression on healthy on expression limited exhibit (FR) ceptors re Folat males1. in diagnosed cancer leading the as reported problem, significant a is cancerrostate SYNTHESIS OF FOLATE-PEG-DOXORUBICIN CONJUGATE, FOLATE-PEG-DOXORUBICIN OF SYNTHESIS 99m Ege University, Faculty ofScience, Biochemistry Department,35100Izmir, Türkiye Tc-FOL-PEG-DOX and the control groups control the Tc-FOL-PEG-DOXand APPLICATIONS AS AN IMAGING AGENT IN CANCER CANCER IN AGENT IMAGING AN AS APPLICATIONS 99m Tc-DOX) were used in biodistribution Tc-DOX)biodistribution in used were International Symposium onDrugResearch &Development 2011 Güliz AK *[email protected] DRD 2011 * , ŞenayŞANLIER O-04 44 - - - 5. 4. 3. 2. 1. monitoring agent. response treatment and agent imaging cancer prostate a as potential radiopharmaceutical high a has conjugate belled eun, t a blee that believed was it sequent, con- a As 160. target/non-targetwasratioorgan addition, In higher. was receptor folate overexpress which prostate and kidney of uptake that showed datas Obtained University. proved by the Institutional Animal Review Committee of Ege o HS, ak .. oaercpo-agtd eiey of delivery Folate-receptor-targeted T.G. Park H.S., Yoo fortargets subcellular as Mitochondria R. Reszka K., Jung and therapeutic Folate-targeted S.A. P.S.,Kularatne Low Hilgenbrink A.R., Low P.S. Folate Receptor-Mediated Drug transfection DNA vitro in Y.EnhancedY., Maitani Hattori 100:247–256, 2004. Release Controlled of Journal conjugate. cin–PEG–folate doxorubi - by stabilized nano-aggregates doxorubicin Reviews 49:87–105. Delivery Drug Advanced anthracyclines. useful clinically Biology 13:256–262,2009. Chemical in Opinion Currentcancer. for agents imaging Pharmaceutical Sciences94(10):2135-2146,2005. of Journal Diagnostics. to Therapeutics From Targeting: lease 97:173–183,2004. prostate cancer and oral cancer. Journal of Controlled Re human in nanoparticles folate-linked novel by efficiency REFERENCES m AND RESEARCH INTO ITS ITS INTO RESEARCH AND 99m cFLPGDX radiola- Tc-FOL-PEG-DOX - ORAL PRESENTATIONS -

han K skin

effects , Barkat A

human

the

ahmood M study

Tariq , Tariq to emulsion

In this study, the instrumental measurements produced han K were were tested. Both base and formulation were applied to the cheeks of human volunteers for a period of four weeks. Dif- ferent mechanical parameters of skin like R0, R1, R2, R3, R4, R5, R6, R7, R8 and R9 were measured by the cutometer and results were evaluated statistically to justify any effect pro duced by these emulsion. Applying ANOVA with respect to R8 and R6 R5, R4, R3, R1, R0, for results that found was it time, R3 while formulation of application the after significant were significant. after of base were and R8 values the application by the formulation regarding various skin mechanical pa- of base. that to comparable were rameters parameters

- - used 45

O-05 DRD 2011 DRD [email protected] * containing Pakistan 63100, Bahawalpur,

technique mechanical

extract , Gulfishan, Haji M Shoaib

* R International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International khta

ioengineering he Cutometer equipped with a 2-mm diameter suction probe is a device suitable for mechanical assessing parameters of the skin. The objec B Naveed Naveed grapefruit T For this purpose, base containing no active material and a and material active no containing base purpose, this For Department of Pharmacy, Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, of Bahawalpur, University Medicine, The Islamia of Pharmacy and Alternative Faculty Department of Pharmacy, formulation containing concentrated crude extract of grape of extract crude concentrated containing formulation tive tive of this study was to determine the effect of grapefruit extract containing emulsion on mechanical parameters of skin while applied by healthy human volunteers. The non- invasive method applied can be useful for investigation of age-related changes. fruit (2%) in the internal aqueous phase (W/O emulsion) ORAL PRESENTATIONS iia aons f oml aie s lcb. Faecal placebo. as saline normal of amounts similar 1. nil fectiveness of a commercial anthelmintic combination (Felo over the world1. This study was performed to evaluate the ef - all from reported been has which anthelmintics, common to parasites of resistanceincreased the to due difficult more becoming is GIP of control but drugs, anthelmintic of use the by achieved been has decades past the over GIP nants Iran. of northwest surroundings, Urmia in ruminants small of spp against m/ k B of BW kg 1ml/5 drenched were animals group treatmentgroups. Then wereforand study the intoselected equal divided two weregoatsrandomly and sheep infectednaturally 100 then technique2 master Mc using examination faecal sexes aged above 4 month were to subjected primarily 2Islamic AzadUniversity- Shabestar Branch, Faculty ofVeterinary Medicine,Dept.ofPathobiology, Shabestar, Iran ® AGAINST AGAINST G , 37.5 mg Levamisole HCl and 50 mg Triclabendazole/ml)50 and HCl Levamisole mg 37.5 , Min BR. and Hart SP. Tannins for suppression of internal of suppression SP.for Tannins Hart and BR. Min parasites. 81:E102-109,2010. JAnimal Sci REFERENCES One thousand free grazing sheep and goats of both STUDY ON A COMMERCIAL ANTHELMENTIC COMBINATION EFFICACY EFFICACY COMBINATION ANTHELMENTIC COMMERCIAL A ON STUDY 1Islamic AzadUniversity- UrmiaBranch, Faculty ofVeterinary Medicine,Dept.ofPathobiology, Urmia,Iran and dendriticum Dicrocoelium spp,Fasciola livestock throughout the world. Control of rumi- of Control world. the throughout livestock to losses production marked cause trematodes liver especially and (GIP)astrointestinalparasites , DICROCOELIUM DENDRITICUM DENDRITICUM DICROCOELIUM , spp FASCIOLA Felonil spp International Symposium onDrugResearch &Development 2011 ®

hra te tes received others the whereas IN SMALL RUMINANTS IN URMIA, IRAN IRAN URMIA, IN RUMINANTS SMALL IN Sohrab R asouli *[email protected] Moniezia 1,* DRD 2011 , Mohammad O-06 46 - these parasites. of control sufficient to necessary is population asites par area every about product, new each of evaluation field that concluded be can it So dose. recommended in least at drug anthelmintic spectrum broad a as tion combina - this on rely to impossible is it and flatworms Company, has not appropriate efficacy against all adult Manufacturer by recommended dose the of istration driticum and cant reduction were about observed signifi- similar no but (P<0/05), study of end the to up sessions sampling other the of levels EPG in decrease significant was there and day 3rd from observed was gate adultworms. investito - werenecropsiedgroup each from animals 5 technique.period,mentioned of Also,using end the at examined was (EPG) faeces of gram per Parasites’egg subjects. groups’ both from treatment after 14 and 7 3, 1, day at rectum from directly taken were samples 2. ruat M ad tes Vtrnr Parasitology. Veterinary others. and GM. Urquhart oiat fet f ramn on treatment of effect Dominant p. 276-281. 2 nd ed. United Kingdom: Blackwell Publishing, Blackwell 2003, Kingdom: Uniteded. S adaghian Moniezia spp. According to results, admin- 2 AND MONIEZIA MONIEZIA Dicrocoelium den- EPG spp Fasciola - ORAL PRESENTATIONS - , < < Cr

< Pb (2007), 5.980 by -1

Jahangir , Biological Oxy - < Mn ,Cl -2 ) and in turnip (0.020 turnip in and ) 4 -1 < Cd , Sajid ue aq rrigated in 2009. H -1 I arachi K , Qamarul Fe. Root vegetable and soil irrigated with IWW with irrigated soil and vegetable Root Fe. < Zn < rain egetables ) in 2008 and Maximum- 2009, concentra respectively. (2008) and 6.80 mg·L ahiri A ater -1 -1 T V Cu Cu < W Co Co samples were examined for pH, Conductivity, Total Dissolved Dissolved Total Conductivity, pH, for examined were samples Solids, Alkalinity, Acidity, Hardness, SO tion of Fe was found in beet leaf 3.798 mg·L gen Demand, Chemical Oxygen Demand, Dissolved Oxygen and heavy Mn,Cu, metals Fe, Cr, Co, (Cd, Ni, Pb and The Zn). samples collected were a over three year period, 2007-2009. The results revealed that metals were in the following order (three year average) in IWW Malir: Ni Malir showed elevated levels of metals except Zn in three mg·L (0.046 radish in Pb and study year mg·L mg·L oot 47 Rafee , Rafee O-07 R DRD 2011 DRD aste in

W Pakistan Karachi-75300, ersiani Iftikhar Ahmed Iftikhar Ahmed V [email protected] * oxicity T ndustrial I International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International etals Muhammad Ali , Muhammad * M

eavy asmeen Y

H n Karachi city, waste water is used for irrigating - veg cause may use etables of Long-term fields. wastewater accumulation of heavy metals in agricultural soils and

Department of Chemistry, Federal Urdu University of Arts, Science and Technology, Gulshan-e-Iqbal Campus, and Technology, of Arts, Science University Urdu Federal Department of Chemistry, I Kousar vegetables. vegetables. Heavy metals such as Cd, Cr, Zn and Mn act as micronutrients at lower concentrations but waste of effect the they elucidate To concentration. become higher at toxic water on heavy metal concentration in vegetables, soil and a region fertilized water, with industrial waste water in Malir was selected for study. The present study is undertaken to determine concentrations of Cd, Co, Cr, Cu, Fe, Mn, Ni, Pb and Zn in waste water, soil and six root vegetables by using the atomic absorption spectrophotometer (AAS). The six vegetables include: investigated beet, carrot, turnip, - rad ish, potato and sweet potato. Industrial waste water (IWW) ORAL PRESENTATIONS stored at different accelerated conditions i.e., 8 were formulations both of Samples prepared. were phase aqueous internal the in extarct 3% containing 2 formulation and extarct 1% containing 1 Formulation emulsion.. w/o of phase aqueous inner the in entrapped wastree, alba Morus on humanskin. 40 ditions at different time intervals for a study period of four of period study a for intervals time different at ditions werepH and measureddifferent atall ductivity storage con - liquefaction, phase separation, centrifugation, electrical con- color, like parameters stability Different creams. these of ity M o 2Department ofPharmacy, Faculty ofPharmacyandAlternative Medicine,TheIslamiaUniversity ofBahawalpur F C+75% RH for a period of four weeks to predict the stabil- Concentrated ethanolic extract of the bark of shoots of shoots of bark the of extract ethanolic Concentrated T Fatima RASOOL ulberry ormulation mulberry extract and comparison of their effects their of comparison and of extract mulberry concentrations different containing creams stable two formulate to was study the of aim he 1University College ofPharmacy, TheUniversity ofthePunjab,Lahore, Pakistan E xtract 1,* International Symposium onDrugResearch &Development 2011 , ShamsUL-HASSAN A nd Barkat AliKHAN S C kin A haracterization nd M *[email protected] C o C, 25 elanin omparison o C, 40 2 2 , HajiMuhammadShoaibKHAN , AtifALİ DRD 2011 O-08 o C, 48 A respect to sensory evaluation. torespect sensory with good were creams the Both skin. human on same are of duced by boththeformulations. pro were pH skin on effects insignificant Statistically tions. formula- both by produced were erythema and melanin in passage of time. Similar effects on skin melanin i.e., decrease differentatthe with werestorageconditions tions observed week to compare any effectproduced by thesecreams. every monitered were pH skin and erythema melanin, skin man volunteers for four weeks. Different skin parameters like hu- of cheeks the to applied were formulations Both weeks. nd 2 Morus alba Morus , AsadullahMADNİ It can be concluded that the effects of ethanolic extract extract ethanolic of effects the that concluded be can It formula - both of pH the in changes (p≤0.05) Significant E O O rythema f f T T (L.) in different concentrations i.e., 1% and 3% and 1% i.e.,concentrations different in (L.) heir wo B E leach ffects 2 2 , Naveed AKHTAR C O reams n H uman O 2 f ,

- ORAL PRESENTATIONS - - - d H ci H O A O O H c i P O n H P ro O d O e l O o H Z N N 3 l C P

, d ci a The The discovery of new polymorphic 2 forms of a pharma- The present study aims to provide a novel polymorph of ceutical. ceutical. Zoledronic acid a crystal forms, sodium Zoledronate salt crystal forms, Amorphous Zoledronate so dium salt, and processes for their preparation. EP patent 200440756693. 2004 Jun 07. Aronhime Aronhime Judith, Lifshitz-liron, inventors; Teva - Pharma l

i s ro u ceutically ceutically useful compound provides a new opportunity to improve the performance characteristics of a - pharmaceuti cal product. zoledronic acid denominated as Form Y, which has - consid erably good flow properties and stability due to low hygro A scopicity. further purpose of the study is to provide a pro cess for producing Form Y with higher reproducibility and economy. material 2. r e o e w - h 49 n o l o O-09 f t sp DRD 2011 DRD n O o 2 ce skeletal Bekir KARLIĞA Su H A Ph

[email protected] ) ) PREPARATION )

2 3 1 l Türkiye Tekirdağ, 59500, Çerkezköy, l C C H

H d i c H a O c i t e O c a International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

e l N o z a N d mi -i

2 oledronic oledronic acid1 (or zoledronate) bisphosphonate is which is designated a chemically type of as - (1-hydroxy-2-imidazol-1-yl-1-phosphono-eth

A NOVEL POLYMORPH OF ZOLEDRONIC ACID AND PROCESS FOR ITS It is used in the treatment of bone disorders, such as Formula I Formula maceutical use. US patent 4,939,130. 1987 February 27. 4,939,130. 1987 February US patent use. maceutical stein. stein. Substituted alkanediphosphonic acids and phar REFERENCES

Jaegg Knut A, Widler L, inventors; Basel and Muchen- Z Deva Holding A.Ş. Çerkezköy API Üretim Tesisi, Organize Sanayi Bölgesi Atatürk Mh., Fatih Blv. No: 26, Karaağaç No: 26, Karaağaç Blv. Mh., Fatih Sanayi Bölgesi Atatürk Organize Tesisi, API Üretim Holding A.Ş. Çerkezköy Deva fractures. fractures. hypercalcemia hypercalcemia caused by cancer, Paget’s disease and osteoporosis and also used to prevent patients from yl) phosphonic acid of the Formula I. yl) phosphonic acid of the Formula 1. ORAL PRESENTATIONS terolandcampesterol levels patientsin withhomozygous fa primaryhypercholesterolemia; andforthereduction sitosof lesterol(LDL-C) andapolipoprotein (ApoB patientsinB) with cho lipoprotein low-density (TC), cholesterol totalelevated indicatedis adjunctiveas therapydietreduction fortheto of statins,combinationwith in or Ezetimibe,aloneabsorption. date of a drug that involves inhibition of intestinal cholesterol alone and in combination with a statin, is the only example to either use for 2002 late approvedin azetidinone,was which fluorophenyl)-3( pies failingto reach theircholesterol goals1. theragreatly,statin- varies on statinspatients all of half with liver.the in biosynthesis ol However, patientresponsethe to the enzyme that catalyzes the rate-limiting step of cholester reductase, HMG-CoA inhibit Statins drugs3. lipid-lowering currentof predominantclass the becomehave statinsfar by 1980s, late the in introduction their Since intestine2. small sis in the liver and (2) absorption of cholesteroldietary in the mechanisms: (1) cholesteroltwo complementary biosynthe 4. 3. 2. 1.

H Bruckert E. New advances in lipid-modifying therapies for SYNTHESIS OF EZETIMIBE: A SELECTIVE CHOLESTEROL ABSORPTION ABSORPTION CHOLESTEROL SELECTIVE A EZETIMIBE: OF SYNTHESIS ztmb, eintd s 1-(4-fluorophenyl)-3( as designated Ezetimibe, sorption. J Med Chem 48, 6035-6053, 2005, and references in vitro evaluation of inhibitors of intestinal cholesterol ab KværnøL, WerderM,Hauser H,Carreira EM.Synthesis and 97-98, 2003. 2: P. Discovery Drug Kirkpatrick J, Rev NatEarl Ezetimibe. 1604, 2002,andreferences therein. 1587- 11: Drugs Investig Opin Expert Ezetimibe. H. Bays and references therein. 2002, 59-66, 97: Cardiology risk. cardiovascular reducing REFERENCES 1 Deva HoldingA.Ş.,Çerkezköy APIProduction Plant,Organize SanayiBölgesi,Atatürk Mh.Fatih Blv. No:26 blood cholesterol level is primarily regulated by regulated primarily is level cholesterol blood total The disease1. cardiovascular for factor risk major a constitute levels blood-cholesterol igh S )-hydroxypropyl]-4( 2 Zentiva HealthProducts, Küçükkarıştıran, 39780Lüleburgaz – Kırklareli, Türkiye International Symposium onDrugResearch &Development 2011 Esen BELLUR ATICI S Karaağaç, 59500Çerkezköy –Tekirdağ, Türkiye -4hdoy phenyl)-2-)-(4-hydroxy * [email protected] R INHIBITOR )-[3-(4- DRD 2011 0-10 50 ------1,* , Mustafa ADIYAMAN stereochemical and chemical purity on a large-scale developedprocessa allowed usto obtain ezetimibe with high intermediatestheliterature,discussed beenhaveinhave we challenge. Although different synthetic routes of ezetimibe and finalproduct with therequired stereochemistry significantisa moleculegiveriseeight to stereoisomers, thesynthesis theof limits0.1%of tify and characterize the present impurities above the accepted PharmaceuticalIngredientsmandatoryidenis to it(API) and of a drug substance is critical for the safety assessment of ActiveHPLC for the purification of the intermediates iliarybased synthesis and used flash chromatography orchiral for this molecule. Many community which led to the development of several syntheses mibehasprompted intense synthetic interest thesyntheticin homozygous familial hypercholesterolemia patientswith inLDL-C and TCreductionof theindicated for milial sitosterolemia. Ezetimibe, in combination with statins, is 7. 6. 5.

Q3A Substances Drug New in Impurities Guideline, ICH of Drugs Ezetimibe. J. Castañer LA, Sorbera RM, Castañer No: TR 2010 00116. 2010 Jan 08, and references therein. azetidin-2-one and processes for producing the same. Appl. 3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl) The novelThestructure potentandbiological activityEzeti of fulfor the preparation of (3 Bellur Atıcı E, Adıyaman M. Zentiva. Novel intermediates 25,2006. (R2), October use the Future 25: 679–685,2000,andreferences therein. therein. 6 . As threeAsasymmetric . carbonsezetimibethein of these routes have utilized chiral aux 2 R ,4 S )-1-(4-fluorophenyl)-3-[(3 4 . 5 .Impurity profile 7 . S )- - - - -

POSTER PRESENTATIONS

POSTER PRESENTATIONS C NMR spectra. 13 H NMR and 1 * Crude Crude compounds were purified by column - chromatog Acknowledgement: This study was supported by raphy raphy by using (diisopropyl ether:methanol (80:20) for 1, ethylacetate:methanol (90:10) for 2, chloroform:methanol (95:5) for 3 and 4. Chemical structures of the compounds by confirmed were Ataturk Ataturk University Research Foundation (Project Number: 2009/317). - 55 H 1 P-001 DRD 2011 DRD [email protected] * C. Corresponding 0 Halise İnci GÜL , Halise İnci Sinan BİLGİNER PYRIDINE-3-YL-PROPENONES International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

halchone compound, 1-(4-hydroxy-3-amino-1- ylmethyl-phenyl)-3-pyridin-3-yl-propenone, was synthesized using p-hyrdoxyacetophenone and Erzurum, Türkiye Chemistry, Department of Pharmaceutical of Pharmacy, Faculty University, Atatürk SYNTHESIS OF 1-(4-HYDROXY-3-AMINO-1-YL-METHYL-PHENYL)-3- C pyridine-3-carbaldehyde in ethanol at 80 NMR results. NMR results. Mannich bases with morpholine (1), piperidine (2), 4-meth- - conven by synthesized were pyrolidine and (3), ylpiperazine The mixture of parafor chalcone compound, tional method. ethanol in heated was amine corresponding and maldehyde for sometime. It was 39.5 h for 3 and 4, 51 h for 1 and 84 h for 2). Heating period was stopped according to TLC and POSTER PRESENTATIONS mined as described in phenyl 3-methoxyphenylin hnl in phenyl 4. 3. 2. 1. changed as phenyl inphenyl aschanged was part aryl followed.The also were structure chemical in Alterationsbiologicalmodificationsindependingactivity on (T47D). cells cancer breast against evaluated were activities (compounds yl-3-(piperidine-1’-yl)propylidene]hydrazinedihydrochlorides totoxic activities of them ofMannich bases with hydrazine. A few studies report the cy encounteredoften problems inthecourse oftherapy3. are agents chemotherapeutic to resistance drug and effects side cancer,severalbreast of treatment the in therapy ation surgery,chemotherapy,radi - as and such endocrine options CYTOTOXICITY OF N,N’-BIS[1-ARYL-3-(PIPERIDINE-1’-YL) PROPYLIDENE] N,N’-BIS[1-ARYL-3-(PIPERIDINE-1’-YL) OF CYTOTOXICITY

B Gul HI, Das U, Pandit B, Li PK. Evaluation of the cytotoxicEvaluationthePK. of PanditLiU, B, Das HI, Gul breast for targets Molecular A. Ullrich E, Zwick J, Bange statis- cancer P.PisaniGlobal J, F, Ferlay Bray DM, Parkin McPherson SteelK, CM, Dixon JM. ABC of breast diseases, cancer cells. Arzneimittelforschung 56: 850-854, 2006. azinederivatives against androgen-independent prostate ity of some mono-Mannich bases and their corresponding cancer therapy and prevention. Nat Med 7: 548-551, 2001. tics, Cancer 2002.CA JClin55:74-108,2005. BMJ 321:624-628,2000. genetics. and factors, risk cancer-epidemiology, breast REFERENCES HydrazonesMannichofbasesformedreactionarethe by HYDRAZINE DIHYDROCHLORIDES AGAINST BREAST CANCER CELLS CELLS CANCER BREAST AGAINST DIHYDROCHLORIDES HYDRAZINE 2 Bilkent University, Faculty ofScience, Dept.ofMolecular Biology andGenetics,Faculty ofScience, Bilkent 1 Atatürk University, Faculty ofPharmacy, Dept.ofPharmaceutical Chemistry, 25240Erzurum,Türkiye) . Despite there are some therapy some are there Despite year1,2. each cases new million a approximately with women among death cancer of cause leading the is cancer reast P3 P8 4-hydroxyphenyl in , Cttxcte o te opud wr deter were compounds the Cytotoxicities of . P1-P8 6,7 wr snhszd n ter cytotoxic their and synthesized were ) and shown at Table 1 (IC P6 P1 Halise İnci , 4-fluorophenylin , 4,5 , 4-methylphenyl, in International Symposium onDrugResearch &Development 2011 . In the present study, N,N’-bis[1-ar P4 G 4-chlorophenyl in , ül 1 P7 , Kaan University, 06800Ankara, Türkiye P2 50 and 4-bromo and , µM). * , 4-methoxy, [email protected] K üçükoğlu DRD 2011 P-002 (T47D) P5 56 ------, 7. 6. 5. 2007/58), Erzurum (Turkey). 2007/58), Erzurum Number: (Project University Ataturk Foundationof Research cer cells (T47D) P1 P3 P7 P6 Compound P4 P5 P2 5-FU P8 Freshny RI. Culture of animal cells: a manual of basic tech- Hansen HB, Nielsen SE, Berg K. Re-examination and fur and Re-examination K. Berg SE, Nielsen HB, Hansen Evalua- KM. King DL, Kirkpatrick E, Erciyas JR, Dimmock nique. New Y 203-210, 1989. 119: Methods Immunol J kill. growth/cell cell measuring for method dye rapid and precise a of development ther EMT6 tumour. Pharmazie 43:614-616,1988. the versus compounds ammonium quaternary related and aminomethylacetophenones of azines some of tion Acknowledgement: *: Noinhibition Table 1: Cytotoxic activity of P Series against breast can- breast against Series P of activity CytotoxicTable 1: 1,* , Rengül-Çetin ork: John& ork: Wiley 2005. Sons, Inc; 4-CH 3-CH 4-CH 4-HOC 4-BrC 4-ClC 4-FC C Ar 3 3 6 OC OC H 3 C 6 6 6 hs td ws upre b the by supported was study This 5 H 6 H H 6 H H 6 6 4 A 4 4 H H 4 4 talay 4 4 Cytotoxicity (IC 2 229.82 114.93 51.59 19.90 16.09 10.05 4.83 7.0 * 50 ), (µM) - POSTER PRESENTATIONS - - and R2, R6, 2 talay A This This study was supported by the value of 5-FU was 42.12 µM. The information 50 , Rengül-Çetin 1 ül Cytotoxic Cytotoxic activities of the compounds synthesized were Acknowledgement: Acknowledgement: ity of some mono-Mannich bases and their - correspond ing azine derivatives against cancer Arzneimittelforschung prostate 56: cells. 850-854, androgen-independent 2006. tion of some azines of aminomethylacetophenones and related quaternary ammonium compounds versus the 43: 614-616, 1988. Pharmazie tumour. EMT6 the management of hepatocellular carcinoma, Nat Clin 4: 424-432, 2007. Oncol Pract Gul HI, B, Li Das Pandit PK.U, Evaluation of the cytotoxic Dimmock JR, Erciyas E, Kirkpatrick DL, King KM. - Evalua Schwartz M, Roayaie S, Konstadoulakis M. Strategies for had more powerful activity than the reference compound compound reference the than activity powerful more had G ment ment procedure for most patients with HCC [6]. investigated investigated against human hepatoma cells (Huh7) since hepatocellular carcinoma (HCC) cells have the high - resis tance against chemotherapeutic agents, treatment options of HCC is very limited and surgery is the only curative treat R7 5-FU. The IC obtained by this study may give direction for further design compounds. of cytotoxic 4. 5. 6. Research Foundation Research of Foundation Ataturk University (Project Number: 2007/58), Erzurum (Turkey). - - - - 57 R6, R1, P-003 DRD 2011 DRD , Halise İnci [email protected] * 1,* R3, 4-hydroxy Türkiye 06800 Ankara, University, R5, 3-methoxyphenyl in üçükoğlu K International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International AGAINST CELLSHUMAN (HUH7) HEPATOMA Kaan R2, 4-methoxyphenyl in R7. Different substituents at different po

ydrazones ydrazones are a special group of compounds in organic chemistry. They have various cal - biologi activities including anticancer and cytotoxic R4, 4-chlorophenyl in Ataturk University, Faculty of Pharmacy, Dept. of Pharmaceutical Chemistry, 25240 Erzurum, Türkiye Chemistry, Dept. of Pharmaceutical of Pharmacy, Faculty University, Ataturk 1

Bilkent University, Faculty of Science, Dept. of Molecular Biology and Genetics, Faculty of Science, Bilkent Bilkent of Science, and Genetics, Faculty Biology of Molecular Dept. of Science, Faculty University, Bilkent 2

vitro vitro antitumoral activity of new hydrazinopyrimidine-5- carbonitrile derivatives. Bioorg Med Chem 14: 366-372, 2006. drazones: drazones: evaluation of anticancer, anti-HIV and - antimi J Med 2004. Chem 39: 113-122, Eur activity. crobial Cosentino Cosentino S, Pisano MB. New alpha-(N)-heterocyclichy new diaryl and triaryl hydrazone derivatives as possible 52: Arzneimittelforschung modulators. receptor estrogen 39-44, 2002. REFERENCES EVALUATION OFEVALUATION THE CYTOTOXICIY OF SOME NEW N,N’-BIS[1-ARYL-3- Cocco Cocco MT, Congiu C, Lilliu V, Onnis V. Synthesis and in Savini L, Chiasserini L, Travagli V, Pellerano C, E, Novellino Pellerano V, Travagli Savini L, Chiasserini L, Pandey Pandey J, Pal R, Dwivedi A, Hajela K. Synthesis of some

(PYRROLIDINE-1’-YL)PROPYLIDENE] HYDRAZINE DIHYDROCHLORIDES H 4-fluorophenyl 4-fluorophenyl in sitions of the phenyl ring may govern the bioactivity, since they have different electronic natures with different Ham- mett values. activities [1-5]. Some new hydrazone bis[1-aryl-3-(pyrrolidine-1’-yl)propylidene]hydrazine compounds, N,N’- dihy drochlorides, were designed and synthesized to find a new leader compounds to develop new compounds. The cytotoxic/anticancer aryl part was changed as phenyl 4-methylphenyl in in phenyl in 3. 2. 1. POSTER PRESENTATIONS 4-ClC which are cytotoxic to ahumanhepatoma cell line. molecules prototypic some find to is strategy long-term our in step first the Hence hepatomas. as to referred often are which carcinomas hepatocellular are cancers liver primary common most The liver)2. the in metastasis which origins system) or secondary malignancies (tumours of extrahepatic hepatobiliary the from (arising tumours liver primary to due mately 20% of cancer-related deaths in the United States are approxi- that example, for considers, one when axiomatic is goals such of importance cancers.Theliver of effects tating devas- the alleviate can which compounds novel of covery dis- the laboratoriesis our in study.goal this major in A med ai- were HEP-3B, line, cell cancer liver against cytotoxicities their of evaluation and dihydrochlorides 2-propene-1-one 2. 1. 2 Yeditepe University, Faculty ofEngineeringandArchitecture, DepartmentofGeneticsandBioengineering,Istanbul, I Stragg RJ, Chang JT. In Textbook of Therapeutics: Drug Therapeutics: of Textbook In JT. Chang RJ, Stragg Dimmock JR, Kumar P. Anticancer and and cytotoxic prop rl at a C was part Aryl erties of Mannich bases. ofMannich Curr Chem4:1-22,1997. Med erties REFERENCES METHYL)-2-PROPENE-1-ONE DIHYDROCHLORIDES AGAINST HEP-3B HEP-3B AGAINST DIHYDROCHLORIDES METHYL)-2-PROPENE-1-ONE 1 6 CYTOTOXICITIES OF SOME 1-ARYL-2-(4-METHYLPIPERAZINE-1-YL- SOME OF CYTOTOXICITIES Synthesis of 1-aryl-2-(4-methylpiperazine-1-yl-methyl)- 1. activities anticancer cytotoxic, have their bases and Mannich ketones unsaturated α,β- that known is t Ataturk University, Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 25240Erzurum,Türkiye H 4 (4), Mehtap TUĞRAK C 3 Ataturk University, Faculty ofMedicine,DepartmentPhysiology, 25240Erzurum,Türkiye 4 H 3 ) in our series. Compounds were Compounds series. our in (5) (2-il) S 6 H 5 , 4-CH (1), International Symposium onDrugResearch &Development 2011 1 , HaliseİnciGÜL 3 C 6 H 4 , 4-CH (2), * 3 [email protected] OC 1,* 6 H , NeşeBAŞAK 4 DRD 2011 P-004 (3), CELLS CELLS Türkiye 58 - HEP-3B cell line city resultscity were shown at Table 1(LC the compounds were determined by MTS method. Cytotoxi- of cytotoxicities and heating conventional by synthesized Erzurum (Turkey). 2010/166), Erzurum Number: (Project Foundation Research University Ataturk Compound al 1. Table phia, p. 1787,2000. Philadel- Wilkins, and Williams Lipincott (editors), DR ley ET, Gour Herfindal ed.In: th 7 Management, Disease and Acknowledgement: 5-FU 2 5 4 3 1 2 , Mustafa GÜL yooiiy f h cmons 15 against (1-5) compounds the of Cytotoxicity 4-CH C 4-CH 4-ClC 4 H C 3 Ar S (2-yl) 3 6 OC H 3 C 6 5 H 6 H 6 hs td ws upre by supported was study This 4 H 4 4 3 , Fikrettin ŞAHİN Cytotoxicity (LC 50 , µM). 48.56 54.93 40.88 24.56 73.44 41.49 50 2 ),

(µm) - POSTER PRESENTATIONS

- 0–∞ and 3 3 zek Ö M. Aykut , M. Aykut 2 3 roğlu E eksaç B , Hakan 1 Acknowledgement: This project was supported by Drug Administration, Center for Drug Evaluation Research (CDER), and Center for Veterinary Medicine (CVM): Guidance for Industry, Bioanalytical Method Validation; 2001. After After validation studies, the method was applied to five US Departmentand US Services,Human and Health of Food eçber , M. Sinan 1 R was was fully validated according to the Food and Drug - Admin istration guidelines bioanalytical for method validation were1.06 ± 0.26 h, 14.35 ± 2.55 L and 102.41 ± 12.21 µg·h/mL µg·h/mL 12.21 ± 102.41 and L 2.55 ± 14.35 h, 0.26 ± were1.06 respectively. caesarean-sectioned women, for Hacettepe University Scientific Research Fund (07 01 301 006). 3. and robust. reproducible repeatable, linear, found caesarean-sectioned women treated/exposed with single intravenous dose of cefepime (1 g Maxipime®) and macokinetic phar profile of cefepime was obtained. Peak serum concentrations of cefepime in caesarean-sectioned women at the arterial port after infusion was 69.23 ± 11.93 µg/mL. The mean elimination half-life, volume of distribution and curve (AUC) concentration-time the under area calculated ır - - - K 59 P-005 DRD 2011 DRD Tuba , Tuba 1 , Sedef 3 *[email protected] emutlu Çalış N CHROMATOGRAPHIC METHOD Pınar , Emirhan International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International 1,* . Therefore dosage rates and - con 1,2 oğan D

OF CEFEPIME LIQUID USING ULTRAFAST VALIDATED A FULLY regnancy alters pharmacokinetic profile of many drugs, because of changing body volume and me tabolism rate EFFECT OF PREGNANCY ON THE PHARMACOKINETIC PROFILES Hacettepe University, Faculty of Pharmacy, Analytical Chemistry Department, Sıhhiye, Ankara, Türkiye Ankara, Sıhhiye, Department, Chemistry Analytical of Pharmacy, Faculty University, Hacettepe 1

Hacettepe University, Faculty of Medicine, Obstetrics and Gynecology Department, Sıhhiye, Ankara, Türkiye Ankara, Sıhhiye, Department, and Gynecology of Medicine, Obstetrics Faculty University, Hacettepe 3 Ayşegül Ayşegül nancy. Best Pract Res Cl Ob. 15: 819-826, 2001. Res Best Cl Ob. Pract nancy. Based Maternal Dose Formulation. Obstet Gynecol 93: 858-868, 1999. REFERENCES Dawes Dawes M, Chowienczyk J. P. Pharmacokinetics in - preg Little B. B. Pharmacokinetics During Pregnancy: Evidence- Pregnancy: During Pharmacokinetics B. B. Little

Hacettepe University, Faculty of Pharmacy, Basic Pharmaceutical Sciences Department, Sıhhiye, Ankara, Türkiye Ankara, Sıhhiye, Department, Sciences Basic Pharmaceutical of Pharmacy, Faculty University, Hacettepe P 2 2. 1. matographic matographic The method. chromatographic separation was performed using 40 mM, pH 3.2 phosphate buffer - contain ing 6% methanol as mobile phase at 0.30 mL/min flow rate. Gradient elution with methanol was applied to get shorter analysis time without any interference from plasma endo gens. During analyses, temperature of and detector set were as 30 °C, 10 °C and 40 column, °C, respectively. samples The detection wavelength was 260 nm and ceftizoxime was used as internal standard. At the optimum conditions, the cefepime analysis from plasma samples was completed in 7 min. Cefepime were extracted from plasma samples using method The (99.3%). recovery high very with acid perchloric centration centration of drugs must be controlled during pregnancy. Here, we identified pharmacokinetic profile in of caesarean and cefepime non-pregnant sectioned women using a simple, rapid, cost-effective and valid ultrafast liquid chro POSTER PRESENTATIONS found to be potent inhibitors of hMAO-A isoform with se with isoform hMAO-A of inhibitors were potent be (5-16) to found C ring substituted and A ring unsubstituted 1. oxidase (hMAO) inhibitory activities oxidase(hMAO) inhibitory monoamine human their for tested were pyrazolines sized Kiran BOPPANA P.K. DUBEY 3 S Venkatesan, J., Sinha, B. N., Ucar, G., Ercan, A. Pyrazoline- A. Ercan, Ucar,G., N., B. Sinha, J., Venkatesan, Med ChemLettMed 18:6362–6368, 2008. Bioorg MAO-inhibitors, as analogues mycobactin based REFERENCES Department ofPharmaceutical Sciences, BirlaInstitute ofTechnology, Mesra, Ranchi835215,Jharkhand,India Compound 16 10 12 11 13 15 14 1 PYRAZOLINE BASED MAO INHIBITORS: SYNTHESIS, BIOLOGICAL BIOLOGICAL SYNTHESIS, INHIBITORS: MAO BASED PYRAZOLINE 8 6 9 7 5 GVK Biosciences Pvt.Ltd.,S-1,Phase-1,T.I.E., Balanagar, Hyderabad 500037,Andhra Pradesh, India rat liver MAO isoforms inhibited pyrazolines carbothioamide 5-diaryl 3, some that reported previously has group our ince 4 Department ofChemistry, J.N.T. University, Kukatpally, Hyderabad 500085,Andhra Pradesh, India 2 Dept. OfBiochemistry, Faculty ofPharmacy, Hacettepe University, 06100Ankara, Türkiye 4 , Vadivelan SANKARAN 5 Informatics, GVK Biosciences Private Limited, 37Sterling Road,Chennai,India 1 , Açelya YALOVAÇ ASLAN 2-OH 2-OH 2-OH 4-OH 4-OH 2-OH 2-OH 4-OH 4-OH 2-OH 4-OH 4-OH International Symposium onDrugResearch &Development 2011 R 1 , twenty–two newly synthe EVALUATION AND SAR STUDIES SAR EVALUATIONAND 2 . Twelvewith molecules 4-OCH 2-OCH 3-OCH 3-OCH 2-OCH 4-0CH 2-CH 3-CH 4-CH 4-CH 2-CH 3-CH R’ 5 3 3 3 3 3 3 , BarijN.SINHA 3 3 3 3 3 3 * [email protected] Gülberk UÇAR 2,* DRD 2011 P-006 , Samiye YABANOGLU ÇİFTÇİ Compound 60 - - 28 30 29 27 26 25 24 23 22 21 decreases both potency andSItowardsdecreases bothpotency hMAO-B. wellas towardsSI as potency hMAO-A; inhibitory however it increase to appeared C ring of Presence (27). one non-selective other the and (22) hMAO-B for one hMAO-A, for tive (21,23-26 molecules eight which in 30), molecules with unsubstituted ring A and without ring C (21- 2. lectivity index for MAO-A (SI MAO-A for index lectivity Zhou M., Panchuk-Voloshina N. A one-step fluorometric one-step A N. Panchuk-Voloshina M., Zhou oxidase activity. Anal Biochem253:169-174, 1997. method for the continuous measurement of monoamine 3 , ArijitBASU 1 N N N X C C C C C C C 3 , Venkatesan JAYAPRAKASH MAO-A 2 , JagannathBEHERA -OCH -CH -CH -CH -Cl -Cl -Cl R - - - ) in the order 10 order the in ) 3 3 3 3 ) were selec were 28-30) NH NH NH O O 3 O O Y S S S -10 4 . Ten. 3 3 , , - POSTER PRESENTATIONS ------l C .H N N 2 H -IMIDAZOL- C H R H C O 06100 Ankara, Türkiye 06100 Ankara,

1 ) I I I ( H O ). O 2 C ) R 5 / P H l A 6 C Sevim DALKARA , Sevim M C 2 ( D gH / H C 2) C C - Nafimidone alcohol was prepared by the reduction of ke of reduction the by prepared was alcohol Nafimidone chro column by realized was products the of Purification Acknowledgement: This project was supported by sis sis of some Oxime 1-(2-naphyl)-2-(imidazole-1yl)etanon and Anticonvulsant Their and Derivatives Ether Oxime and 2001. 421-433, 36: Chem Med J Eur Activities. Antimicrobial sis, anticonvulsant and antimicrobial activities of some new 2-acetylnaphthalene derivatives. Bioorg Chem 18(8): 2902-2911, 2010. & Med Karakurt A, Dalkara S, Özalp M, Kendi E, Stables J.P. Synthe J.P. Stables E, Kendi M, Özalp S, Dalkara A, Karakurt Karakurt A, Özalp M, Dalkara Işık S. Ş, Synthe Stables J.P, D ; 5 1)

H ton ton group in nafimidone. Esters of nafimidone alcohol were synthesized by acylation of the alcohol group with carbox ylic acids. matography and crystallography. Structural elucidation of the purified compounds was realized by IR, 1H-NMR, MASS spectral and elementary analysis data. Antifungal and - anti bacterial activities of the compounds were tested by micro dulution method against three fungi and four bacteria, two are Gr (+) and two are Gr (-). Ampicilin and fluconazole were used as reference compounds for antibacterial and - antifun gal activities respectively. Most of the compounds showed activities. antimicrobial Hacettepe University Scientific Research Fund (HÜBAB 3. 4. 010D06301003 6 C N 4 ------61 H 6 N ). P-007 C DRD 2011 DRD 2 III - , Didem KART ; H 1 5 C H H H 6 C O C 2 H C ) I - I ; ( 3 Department of Pharmaceutical Chemistry, Department of Pharmaceutical H 1 . Structural similarities . similarities Structural C 2 - ANTIMICROBIAL COMPOUNDS : antifungals prompted us prompted antifungals 4 R H B . . In as this a study, continua a N 3,4

l -azole -azole C H Mustafa Fahir ACAR Fahir Mustafa .H 1 N International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International N 2 H C ) ) and its active metabolite nafimidone al I C O

derivatives of nafimidone and nafimidone alcohol alcohol nafimidone and nafimidone of derivatives ntifungal ntifungal infections are the frequent threatening and problem life for transplant recipients, cancer and AIDS patients receiving broad spec ) ) ) are the well-known representatives of (arylalkyl) I (

II Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Hacettepe University, Hacettepe of Pharmacy, Faculty Microbiology, Department of Pharmaceutical REFERENCES 1-(Naphthylalkyl)-1H-imidazole 1-(Naphthylalkyl)-1H-imidazole derivatives, a new class of anticonvulsant agents. Eur J Med Chem 24(1): 67-74, 1981. tive sythesis and antifungal activity of (Z)- trans-3azolyl- (Z)- of activity antifungal and sythesis tive oxime ethers. 2-methylchromanone Bioorg & Med Chem 12: 5881-5889, 2004. Nafimidone Nafimidone ( Emami S, Falahati M, Banifatemi A, Shafiee A. Stereoselec A. Shafiee A, Banifatemi M, Falahati S, Emami Walker Walker K.A.M, Wallach M.B, Hirschfeld D.R. 2

1-YL)-1-(NAPHTH-2-YL)ETHANOL ESTER DERIVATIVES AS POTENTIAL A SYNTHESIS AND STRUCTURAL OFELUCIDATON NEW 2-(1 1. 2. trum antibiotics. Therefore, the efforts to develop more ef- area popular are agents antifungal systemic safer and fective medicinal chemists1. for cohol ( compounds anticonvulsant imidazole of these compounds of with these compounds to study on their antifungal/antibacterial activities; we found activities; to on study antifungal/antibacterial their various that activities antimicrobial exhibit tion of our interest on (arylalkyl)imidazole derivatives, we de we derivatives, on (arylalkyl)imidazole interest of our tion nafi of derivatives ester alkyl/arylalkyl/aryl new some scribed ( compounds antimicrobial potential as alcohol midone POSTER PRESENTATIONS is represented by the occurrence of occurrence the by represented is goal this achieving in difficulty a However,sometimes, it. of step first the is expression its then and gene, of cloning and isolation that, For discovery. drug for opportunities unique of metabolism for important is which proteins new of Exploration noteworthy. is discovery drug Thus, diagnosis. rapid to addition in treatment adequate is programs control malaria of objective main the Currently, OPTIMIZATION AND COMPARATION OF NESTED AND SEMI NESTED PCR PCR NESTED SEMI AND COMPARATION NESTED AND OF OPTIMIZATION M WITH CONVENTIONAL PCR FOR ISOLATION OF PLASMODIAL ENOLASE ENOLASE PLASMODIAL OF ISOLATION FOR PCR CONVENTIONAL WITH 2 Malaria&Emerging Parasitic DiseasesLaboratory, Parasitology Department,NationalCentre ofMicrobiology, Instituto deSaludCarlos III,Cra. MajadahondaPozuelo Km.2,Majadahonda,28220Madrid,Spain ol t cnrbt t is oto i necessary. is control its to contribute to tools new developmentof the so and infections sitic alaria is one of the world’s most prevalent para - Venhar 1 Department ofBiology, Faculty ofSciences, Firat University, Elazığ23119,Türkiye Ç International Symposium onDrugResearch &Development 2011 el İ k 1,* , Irmak

lack of lack offers Plasmodium İ çen genomic DNA genomic * [email protected] 1 , JoseMiguel DRD 2011 P-008 GENES 62 lase gene. nested and semi nested PCR for isolation of Plasmodial eno with conventional PCR. At the same time, we have optimized result take couldn’t we although PCR, nested semi and ed the five species of among worldwide parasites malaria common most second Plasmodium falciparum Plasmodium ventionalPCR. Weof succesfullygenes isolatecould enolase we have tried nested and seminested PCR in addition to con- Thus, levels. parasitemia low on depending concentration R ubio 2 , Ömer Plasmodium and M unzuro P. that infect humans, with nest vivax, which are the first and first the are which vivax, Ğ lu 1 - - POSTER PRESENTATIONS lu Ğ unzuro M , Ömer cally by DNA- and RNA-specific nucleases, it is much more laboratorythe in molecules RNA native with work to difficult because RNAases are nearly ubiquitous. Thus, we prefered to genomic DNA instead of RNA for gene cloning and then its expression. But, there are in introns most of genes in - Api complexan. We used PCR based site-directed mutagenesis for removal of the introns in genes. Initially, we generated by fragments exon PCR, then we connected fragments exon to one another by a short PCR cycle. The resulting product fusion amplified further by PCR. This approach especially dif- is which parasites from genes of isolation for used be can be obtained their RNA. ficult to k İ - - - 63 el Ç are P-009 Plas DRD 2011 DRD - resis rug EXPRESSION drugs [email protected] * Venhar , Venhar * spp. spp. which are re çen İ Babesia Irmak International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Eimeria, Elazığ 23119, Türkiye University, Firat of Sciences, Faculty Department of Biology, spp., spp., which cause severe human malaria,

, Theileria

he phylum Apicomplexan’s members such as Apicomplexan’s he phylum modium and THE USE OF SITE-DIRECTED MUTAGENESIS FOR REMOVAL OF THE INTRONS IN APICOMPLEXAN’S GENES: A NEW APPROACH FOR GEN T sponsible for economic losses, result in profound medical, d of development The effects. economic and social, tance tance in Apicomplexan mean that more effective traction are required for studies on gen expression. However, However, expression. gen on studies for required are traction RNA molecules are generally less stable than DNA. In addi- - enzimati degraded are RNA and DNA of both although tion, urgently urgently needed. The gen expression is an important stage to identify proteins which can be potential drug targets in ex RNA therefore and analysis RNA parasites. Apicomplexan POSTER PRESENTATIONS 3. 2. doxycycline effect on the viability of Caco-2 cells. Accordingcells. Caco-2 of viability the on effect doxycycline cells were investigated. MTT test was performed for studying Caco-2 through formulations liposome and solution cline doxycy of studies transport cells, Caco-2 on doxycycline of effects cytotoxic Thecultures. cell model as used were cells 1. n mmrn tasot studies. transport membrane and permeability passive in model (BBB) barrier blood-brain tro vi- in an as used increasingly are that absorption, drug oral make to used widely are which cells, cancer colon human

ınvestıgatıon D Beck RCR, Pohlmann AR, Hoffmeister C, Gallas MR, Collnot E, J.Leyden,MD. James Smith,MD, Kelly D.Vargas-Estrada,J.Gracia-Mora. aoatcecae mcoatce: orlto between Correlationnanoparticle-coated microparticles: SvhaeferEF, Guterres SS,Lehr CM.Dexamethasone-loaded 27(9): 1329-1342,2005. review systematic A minocycline: and cline cline an injectable long-acting parenteral formulation of REFERENCES development hyclate in calves 1 Erciyes University, Faculty ofPharmacy, Dept.ofPharmaceutical Technology, 38039Kayseri,Türkiye 2 Gazi University, Faculty ofPharmacy, Dept.ofPharmaceutical Technology, 06330Ankara, Türkiye aiu tp o infections. of type various overcome to used been has It tetracycline. from derived antibiotic, semi-synthetic a is oxycycline . Researchin Vet. Sci. 84: 477-482, 2008 International Symposium onDrugResearch &Development 2011

Çiğdem YÜCEL transport 3 Food andMouthDiseasesInstitute, 06520Ankara, Türkiye

of hraoiei suy of study Pharmacokinetic 3,4,5

. In this study, Caco-2 Caco-2 study, this In . lıposome 1,2 Cc- cls are cells Caco-2 . doxycy of Safety . Clin. Therap.Clin. . 1,* , ZelihagülDEĞİM

* propertıes [email protected] doxycy DRD 2011

P-010 formulatıon 64 - - - .

5. 4. predictive. and useful be to found was experiments vitro in for model culated as0.881±0.030,2.82±0.15(n=3)respectively. 76.5% (n=3). Apparent coefficientspermeability (k) were cal- 77%, and 67.4% 74.5%, be to found was cells Caco-2 of side some formulations transported through apical to basolateral in 10µg/mLdoxycycline concentration. totest the results,MTT cell wasviability found to be efficient Artursson Artursson P, Palm K, Luthman K. Caco-2 monolayers in ex Hurst L, Fenart R, Cecchelli N, Borg M, Ball P, Garberg Adv Reviews 46:27-43,2001. DrugDel perimental and theoretical predictions of drug transport. 19: 299-334,2005. Vitro in Toxicology barriers. blood-brain he fort models D,mirovic Terasaki T,JO,vitroÖsterbergÖberg T,In al. et Stani- TJ, Raub JE, Nilsson A, Mabondzo T, Lindmark RD, monolayers. Eur J of Pharm and Biopharm 67: 18–30, 2007. releasevitrodrugtransportdrugandin acrossCaco-2cell For conclusion, the use of Caco-2 cell monolayer as a BBB The cumulative amount of doxycycline solution and lipo

2 through , Şükran YILMAZ

doxycylıne

caco 3 -2 cell

and

lıne

- - POSTER PRESENTATIONS - - ) and the AAI WIN 55,212- WIN AAI the and (1) -THC 9 Chemical structures of ∆ of structures Chemical These These features have been used in the design of our Yang, Yang, B.; Showalter, V.M.; Abood, M.E.; Martin, B.R. Drug Depend 60, 133, 2000. Alcohol Aung, Aung, M.M.; Griffin, G.; Huffman, Wu, J.W.; M.-J.; Keel, C.; 2 (2) showing the proposed overlapping moieties involved as a, b and c. denoted interaction, in receptor cannabimimetic aminoalkylindole based naphthylamines, where our compounds consist of a naphthalene ring, car bonyl group and a second naphthalene ring with substituents at the 5- and 8-positions, instead of a morpholinoethyl focus to is study this for rationale The chain. carbon or group the specific effects of 5- and 8-substitution, and eventually examine the resulting physiochemical and biological prop erties. The synthesized compounds will be using characterized spectroscopic techniques including UV-Vis, FTIR and photoluminescence.v 2. - 65 Dürdane ÇANDAR ZENGİN, Dürdane , Hüseyin P-011 * DRD 2011 DRD DERIVATIVES *[email protected] -tetrahydrocannabinol -tetrahydrocannabinol 9 D -THC allows -THC for hydrophobic 9 D International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International -THC -THC is fulfilled by the naphthalene 9 D Gülay ZENGİN, Adem MERT Gülay ZENGİN, -THC overlaps with the carbonyl moiety of carbonyl the with overlaps -THC 9 D

he synthesis of cannabimimetic aminoalkylindole based naphthylamine derivatives is in progress, where substituents at the 5- and 8-positions of CANNABIMIMETIC AMINOALKYLINDOLE BASED NAPHTHYLAMINE The The steric requirement for receptor interaction of the Gaziantep University, Faculty of Science and Literature, Department of Chemistry, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Chemistry, and Literature, of Science Faculty University, Gaziantep SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL PROPERTIES OF

1,2 T Med Chem Lett 4, 563, 1994. Med Chem Lett REFERENCES Huffman, J.W.; Huffman, Dai, J.W.; D.; Martin, B.R.; Compton, D.R. Bioorg -THC) and -THC) aminoalkylindoles (AAI), three discrete regions 9 1. (D droxyl group of group droxyl ring of AAIs. Potential hydrogen bonding by phenolic hy interaction which may be facilitated by the morpholinoethyl morpholinoethyl the by facilitated be may which interaction group of AAIs. Further this morpholinoethyl group may be replaced by carbon chains as chains of four to six carbons optimal affinity. produce of interaction with cannabinoid receptors have been - identi fied. cyclohexene cyclohexene ring of AAIs and a C-3 alkyl chain of the naphthalene ring will be examined and manipulated in accordance to their size and electronic effects. Thus far as a result of early molecular studies of POSTER PRESENTATIONS we produced functionally active recombinant D-arabinitol D-arabinitol recombinant active functionally produced we study, this In marker. diagnostic important an as described is D-arabinitol findings, these on Based therapy. antifungal with decreases D-arabinitol serum of concentration the and controls uninfected in than candidiasis invasive hu- with mans in higher are concentrations D-arabinitol serum that pathogenic arabinitol, five carbon sugar alcohol is a metabolite of several I P diagnosis of invasive candidiasis is very important. D- important. very is candidiasis invasive of diagnosis accurate and early Therefore, years. recent in creased in- dramatically has candidiasis invasive of ncidence roduct Department ofBiochemistry, SchoolofPharmacy, University ofHacettepe, 06100Ankara,Türkiye pce. eea suis ae shown have studies Several species. Candida I on International Symposium onDrugResearch &Development 2011

recomb Kevser E scher I Bİ nant beroğlu DRD 2011 P-012 66 D- I ch used for determination levels ofD-arabinitol inserum. suggest that recombinant enzyme, produced in results kDa. These 30 at band SDS-PAGEa by showed zyme ic activity, 25 U/mg). Analysis of the purified recombinant en- chromatographyaffinity (Purification fold, 5000- fold; specif- dye-ligand by purified was rArDH levels. D-arabinitol serum in (rArDH) dehydrogenase search Fund. Re University Hacettepe the from 002) 301 01 (05 grant arab , ÖzdenTACAL I Acknowledgement: a C ol I nol I

dehydrogenase hs td ws upre b a by supported was study This for enzymatic detection of detection enzymatic for E.coli E.coli can be I n

- POSTER PRESENTATIONS - - - days) based doi:10.1016/j. th days, in each gender th and 120 th , 60 th and 120 th , 60 th Food Food Chem Toxicol PMID:15304303. fct.2004.05.001. 42: 1563–1571. nutrition interface: The gap is narrowing. Eur J - Pharma col 651: 1–8. doi:10.1016/j.ejphar.2010.11.007. PMID: 21114994. istry and hematology historical data in control Sprague- Dawley rats from pre-clinical toxicity studies. Toxicol Exp PMID: doi:10.1016/j.etp.2005.10.002. 213–219. 57: Pathol 16343876. Georgıou, Georgıou, N.A., Garssen, J., Wıtkamp, 2011. R.F. Pharma– Petterino, C., Argentino-Storino, A. 2006. Clinical chem- 4. 5. her groups and/or periods (30 and group, 8 rats were sacrified and then 1-1.5 ml of fresh blood samples were used at automatic hematological assay analyzer for complete blood counts. Among control and ot on hematologic parameters, statistical significances and gender their were to accordance in tabulated and determined This study shown that, minimum 1 % rate differences. group (~25-40 apricot/day 3-5 briefly or period days 30 least at and g/day) consumption of organic dried apricot may be remar each gender. kably health for human benefical for body weights of rats were determined, as 320.6 g for male rats (n=120), and 209.7 g for female rats (n=120) at the be ginning of At study. 30 - 67 P-013 DRD 2011 DRD İsmet YILMAZ [email protected] PARAMETERS IN RATS L. Kabaaşı spp.) consumption International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Department of Pharmacology, Faculty of Pharmacy, University of İnönü, 44280 Malatya, Türkiye Türkiye of İnönü, 44280 Malatya, University of Pharmacy, Faculty Department of Pharmacology, he main purpose of this study was to investigate the medicinal importance of organic dried apricot (Prunus armeniaca THE EFFECTS OF ORGANIC DRIED APRICOT ON THE HEMATOLOGIC T Cadmium-induced Cadmium-induced changes in lipid peroxidation, blood biochemical hematology, parameters and semen quality of male rats: protective role of vitamin E and β-carotene. methyl parathion in rats. J Hazard Mater 153: 1117–1121. 153: Mater Hazard J rats. in parathion methyl PMID: 17964717. doi:10.1016/j.jhazmat.2007.09.067. al properties of main Malatya apricot (Prunus armeniaca L.) varieties. Food Chem 107: foodchem.2007.08.052. 939–948. doi:10.1016/j. REFERENCES El-Demerdash, F.M., Yousef, M.I., Kedwany, F.S. et al. 2004. F.S. M.I., Kedwany, Yousef, El-Demerdash, F.M., Celık, I., Suzek, H. 2008. The hematological effects of - composition Some 2008. A. Topcu, I., Karabulut, E.B., Akın, 3. 2. 1. based on hematologic parameters and the second purpose was to determine best ratio and/or period of organic dried this In human. and/or rats in diet of supplementation apricot study, 120 male and 120 female Sprague Dawley rats were divi- randomly were rats twentyfour gender, each From used. (cont I Group follows: as (n=24/groups) groups five into ded rol) were fed with standard rat group chow, II were fed with and % 5 fed were IV group %, 2.5 with fed were III group %, 1 V group were fed 10 % organic dried apricot supplemented to standard diet were given for 120 days study period. The POSTER PRESENTATIONS were determined 320.6 g and 209.7 g respectively. At 30 At respectively. g 209.7 and g 320.6 determined were rats female and male of weights body the study, of ginning be the At period. study days 120 for given were diet dard (ODA)apricot organicdried fed% 10 supplemented tostan- were (n=24) V Group and % 5 fed were (n=24) IV Group %, 2.5 with fedwere (n=24) III Group %, 1 with fedwere (n=24) II Group chow, rat standard with fed were n=24) (control, I Group follows: as groups five into divided randomly were rats 24 gender, each From used. were rats Dawley Sprague female 120 and male 120 study, this In rats. in levels pacity ca- antioxidant total and parameters biochemical serum on 4. 3. 2. 1. THE EFFECTS OF APRICOT ON BIOCHEMICAL PARAMETERS AND TOTAL AND PARAMETERS BIOCHEMICAL ON APRICOT OF EFFECTS THE Bazzano LA, Li LA, Bazzano TY,fruit,of veg Intake FB Hu - Joshipura KJ, and recommendations Nutrition A Diabetes American additive food a of effect Physiological MS Al-Shinnawy prop compositional Some TopcuI, A Karabulut EB, Akın Diabetes Care 31: 1311-1317,2008. women. in diabetes of risk and juices fruit and etables, 2008. 61-78, 31: Care Diabetes Association. Diabetes American the of statement position a diabetes: for interventions 2009. rats. albino male of parameters biochemical and hematological some on eties. Food Chem107:939–948,2008. (Prunusapricot Malatya armeniaca main of erties REFERENCES T 3 Center ofExperimental AnimalsResearch andProduction, L. Kabaaşı spp.) at different ratios and/or periods periods and/or ratios different at spp.) Kabaaşı L. armeniaca (Prunus apricot organic dried of effects investigatethe was study this of purpose main he İsmet YILMAZ 1 Department ofPharmacology, Faculty ofPharmacyUniversity ofİnönü,44280Malatya, Türkiye 2 Department ofBiochemistry, Faculty ofMedicineUniversity ofİnönü,44280Malatya, Türkiye Egypt Acad J Biolog Sci 2(1): 143-151, 2(1): Sci Biolog J Acad Egypt International Symposium onDrugResearch &Development 2011 ANTIOXIDANT CAPACITY LEVELS IN RATS IN LEVELS CAPACITY ANTIOXIDANT 1,* ,

Yusuf TÜRKÖZ * 2 [email protected] , İsmailTEMEL L.) vari- L.) DRD 2011 P-014 th 68 - - . 9. 8. 7. 6. 5. 60 rameters, beneficalfor remarkably eachgender. pa- biochemical important on based be may consumption least 30 days period or briefly 3-5 apricot/day (~25-40 g/day) their genderandgroup differences (Table2, 3). to accordance in tabulated and determined were nificance sig- statistical parameters biochemicaal on based days) 120 Among controls and other groups and/or periods (30, 60 and obtained serum samples were used for biochemical analysis. r.p.m.3000 at centrifuged samples and blood min then for5 anticoagulant, any without tubes centrifuge into collected fied, 7-10 ml blood were drawn by intracardiac puncture and th Kahlon TS, Smith GE In vitro binding of bile acids by ba - by acids bile of binding vitro In GE Smith TS, Kahlon Pharma–nutrition RF Wıtkamp J, Garssen NA, Georgıou and E vitamin of effect Antioxidant FM El-Demerdash in- Preventionthe Diabetes in Program Reduction Group Celık I, Suzek H The hematological effects of methyl para- nectarines. Foodnectarines. Chem101: 1046–1051, 2007. and apricots pears, grapes, pineapple, peaches, nanas, 2011. interface: The gap is narrowing. Trace Biol18:113–121,2004. ElemMed J aluminium. to exposed rats in parameters biochemical and activities enzyme peroxidation, lipid on selenium metformin. 346:393–403,2002. N Engl JMed or intervention lifestyle with diabetes 2 type of cidence thion inrats. JHazard Mater 153:1117–1121,2008. This study results shown that, minimum 1% rate and at and rate 1% minimum that, shown results study This and 120 2

University ofİnönü,44280Malatya, Türkiye ,

Şule GÜRSOY th days each gender and groups, 8 rat were - sacri 2 , ZümrütDOĞAN Eur J Pharmacol 651: 1–8, 3 POSTER PRESENTATIONS -

Spect S S 1,* H N R H N O S C H N 2 S H Studies Studies on the synthesis of 5-(p- C 2 S H C N H 2 N H-NMR, mass spectroscopy and elemental 1 O C S H Ayşegül KARAKÜÇÜK İYİDOĞAN KARAKÜÇÜK , Ayşegül N 1 R HA. Synthesis and antimicrobial activityde rhodanine of antimicrobial and Synthesis HA. J Med Chem 32: 759-762, 1997. Eur rivatives. aminobenzylidene)-rhodanine and its properties. A 59: 651-656, 2003. Chim Acta Part Habib NS, Ridal SM, Badaweyl EA, Ghozlanz HTY, Fahmyl Tang E, Yang G, Yin J. the literature, the then literature, substitue isothiocyanates were added to the biologically active amines due to obtain thiourea derivates. The chemical structures of compounds were elucidated using IR, analysis. analysis. 3. 4. - 69 P-015 J Am DRD 2011 DRD *[email protected] Some - phenyl Bedia KOÇYİĞİT KAYMAKÇIOĞLU Bedia KOÇYİĞİT , Emine Elçin ORUÇ EMRE ORUÇ , Emine Elçin 1 DERIVATED FROMDERIVATED RHODANINE International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

İnci Nejla DAĞDEVİREN İnci Nejla SYNTHESIS AND CHARACTERIZATION SOME NOVEL THIOUREA Gaziantep University, Faculty of Arts and Sciences, Department of Chemistry, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Chemistry, of Arts and Sciences, Faculty University, Gaziantep

1 t is well known that compounds containing substitue thiourea have been reported to posses antimicrobial, antidiabetic, antibacterial, anticancer activities [1-3]. Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 81010 İstanbul, Türkiye 81010 İstanbul, Chemistry, of Pharmaceutical Department of Pharmacy, Faculty University, Marmara 2 OL, Bambas L, Youmans AS. Youmans GP, as inhibitors of JSP-1. Bioorg Med Chem Lett 15: 3374- 3379, 2005. REFERENCES thiourea derivates and their antituberculos activity. Chem Soc 80: 2205-2217, 1958. In this research was composed of two parts by us- Doub L, Richardson LM, Herbst DR, Black ML, Stevenson Cutshall Cutshall NS, O’Day C, Prezhdo M. Rhodanine derivatives I 2. 1. ing general synthesis methods. In this first part 5-(4-nitrobenzilydene)-2-thioxo-1,3-thiazolidine-4-one of study, was - 4-nitroben with rhodanine condensation the by synthesized reduction the After [4]. literature the to according zaldehyde thio amines, of compound corresponding to group of nitro Also, Also, it was thought that thiourea compounds combining with rhodanine ring could exhibit suitable pharmaceutical side effects. undesirable properties and avoid substituted to addition the by obtained were derivatives urea Inisothiocyanates. 3-(2-aminoethyl)-2- partsecond of study, thioxo-1,3-thiazolidine-4-on was synthesized by reactions according hydrochloride rhodanine2-chloroethylamine and POSTER PRESENTATIONS 1. sre o nw hora eiaie wr otie b the by obtained were derivatives thiourea new of series a development.Therefore, drug new of aim the with thesized sive activities - antihyperten and anticonvulsantanti-HIV, antituberculosis, antifungal, anticancer, antiflammatory, analgesic, bacterial, anti- antimicrobial, as such properties biological interesting 2. D lse A, ogt R. usiud heterocyclic Substitued RM. Doughty AC, Glasser ensh , auzzk , akwt D atsr B. Tantisira D, Ralkowitz B, Matuszczak G, Heinisch n hs eerh oiia tiue drvtvs ee syn- were derivatives thiourea original research, this In REFERENCES 1031-1033, 1962. 51: Sci Pharm J activity. I.Antitubercular thioureas. 210, 1997. ticonvulsant activity. Archiv der Pharmazie 330: 207- an- their of evaluation and derivativesthiourea and urea N-aryl-N-heteroaryl-substituted of Synthesis Gaziantep University, Faculty ofArtsandSciences, DepartmentofChemistry, 27310Gaziantep, Türkiye İnci NejlaDAĞDEVİREN, EmineElçin ORUÇEMRE,Ayşegül KARAKÜÇÜKİYİDOĞAN SYNTHESIS AND CHARACTERIZATION SOME NOVEL THIOUREAS THIOUREAS NOVEL SOME CHARACTERIZATION AND SYNTHESIS opud, ay f hc kon o possess to known which of many compounds, thiourea of classes different the on vestigations in- intense been have there years recent uring 1-4 . International Symposium onDrugResearch &Development 2011 DERIVATED FROM HETEROCYCLIC AMINES HETEROCYCLIC DERIVATEDFROM *[email protected] DRD 2011 P-016 70 IR, using illuminated were compounds of structures isothiocyanates. Chemical different with benzoxazol and pyrimidine, isoxazole as such amines heterocyclic of condensation Cl 3. 4. 1 aau S Kyaçol B Tku Z Aıığu F, Arıcıoğlu HZ, Toklu B, Kaymakçıoğlu S, Karakuş Tian Z, Plata DJ, Wittenberger SJ, Bhatia AV. A gener zoles. Tetrahedron Lett 46:8341-8343.2005. N-alkyl-2-aminobenzoxaand - N-aryl- of synthesis al Chem Life 342:48-53.2009b. Sci Pharmazie der Archiv azole-2-yl)phenyl]thioureas. new of activity antituberculosis and Synthesis S. Rollas H-NMR, massspectroscopy andelemental analysis. - N-phenyl-N-[4-(5-alkyl/arylamino-1,3,4-thiadi N O F N H C S N H

R O Cl N N H N N C S N H N H R * C S N H R - POSTER PRESENTATIONS 1

, 1 R Staphylococcus Staphylococcus H N H N 2 S H N R,R'= substituents various Emine Elçin ORUÇ EMRE ORUÇ , Emine Elçin 1,* R , Mehmet ÖZASLAN 2 - antimicrobi vitro in and Synthesis (). K., Tiwari A., Soni, A., al benzaldehyde studies of some new 3-[phenyldiazenyl] N-phenyl thiosemicarbazones. J Enzym Inhib Med Chem 23(1), 77-81, 2008. Das Balzarini U., J., De E., Clercq, Dimmock, J. R., (). 1-aryl- methyl-2,3-dioxo-2,3-dihydroindole thiosemicarbazones J as and leads cytotoxins developing fro anticonvulsants. Enzym Inhib Med Chem 24(2), 537-544. 2009. Halve AK., Bhashkar B., Sharma V., Bhadauria R., Kankoriya R., Bhadauria V., Sharma B., BhashkarAK., Halve Karkı SS., Bahadurıa VS., Rana V., Kumar S., Subbaro PG., ATCC 25322, 25322, ATCC coli (Escherichia bacteriaGram-negative against Psedoumanas aeruginosa ATCC 25853) and Gram-positive bacteria (Enterococcus faecalis 25923, ATCC ATCC 29212) was aureus determined ATCC by microdilution broth (MIC) inhibitoryminimum were The concentrations method. that compounds the of concentrations lowest the as defined visible growth. prevented 4. 5. - - - - 71 P-017 DRD 2011 DRD . 1-5 Derya İŞLER , Derya 2 [email protected] * AND ANTIBACTERIAL ACTIVITY Ayşegül KARAKÜÇÜK İYİDOĞAN KARAKÜÇÜK , Ayşegül 1 İbrahim Halil KILIÇ İbrahim International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International C NMR spectral data and elemental 13

H NMR,

1 Zeliha MERCAN hiosemicarbazones hiosemicarbazones are belong to a large group of are activities biological whose derivatives thiourea a function of parent aldehyde and ketone moiety. Gaziantep University, Faculty of Arts and Sciences, Department of Biology, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Biology, of Arts and Sciences, Faculty University, Gaziantep In vitro antibacterial activity of these compounds 2 Gaziantep University, Faculty of Arts and Sciences, Department of Chemisty, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Chemisty, of Arts and Sciences, Faculty University, Gaziantep 1 T In this study we prepared thirteen thiosemicarbazone Cardenas Cardenas BDM., Naqvi F. Azam A. Synthesis and in vitro antiprotozoal activity of 5-nitrothiophene-2-carboxalde thesis and evaluation of β-thiosemicarbazone derivatives. Bioorg Med Chem Lett anti-HIV activity of 15, 4451-4455, 2005. isatin rivatives. Eur J Med Chem 45, 3453-3458, 2010. Eur rivatives. hyde thiosemicarbazone derivatives. Bioorg Med Chem 12, 3475-3478, 2002. Lett titumor activity of liquiritigenin thiosemicarbazone de REFERENCES Bharti N., Husain K., Garza MTG., Vega DEC., Garza JC., Bal TR., Anand B., Yogeeswari, P. Sriram D. - Syn Hu K.,ZH., Yang Pan SS., Xu HJ., Ren J. Synthesis and an- THE NOVEL THIOSEMICARBAZONES: SYNTHESIS, CHARACTERIZATION ized by UV, ized IR, by UV, derivatives derivatives in good yields by the reaction of ing - correspond 4-substituted phenylthiosemicarbazides with various heterocyclic and aromatic aldehydes in appropriate solvent. Structures of synhesized compounds have been character 3. 2. 1. analysis. analysis. Especially, Especially, heterocyclic and aromatic thiosemicarbazones have attracted considerable pharmaceutical interest due to antipro antimalarial, antitumor, antiviral, antimicrobial, their tozoal, anticonvulsant and antituberculosis activities and antituberculosis anticonvulsant tozoal, POSTER PRESENTATIONS vities - acti antitubercular antiinflammatory, analgesic, antifungal, 2. 1. des, which synthesized by reaction of ethyl 2-{[(4-substitu - ethyl of reaction by synthesized which des, hydrazi- and benzaldehyde 4-substitued with condensation from obtained been have derivatives These activite. robial benzamide derivatives were synthesized to evaluate antimic tutedbenzylidene)hydrazinyl]-1-oxo-3-sulfanylpropan-2-yl} 4-substituted of series new a Therefore, Bhandari SV, Bothara KG, Raut MK, Patil AA, Sarkate AP, Sarkate AA, Patil MK, Raut KG, Bothara SV, Bhandari Koçyiğit-Kaymakçıoğlu B, Koçyiğit-Kaymakçıoğlu and Schiff bases of Diclofenac acid as Nonucerogenic De of studies Novel Ulcerogenicity and Analgesic flammatory, Antiin - of Evaluation and Synthesis Desing, MokaleVJ. 41(11): 1253-1261,2006. Chem Med J Eur activity. structure-antituberculosis their of study the and hydrazide-hydrazones novel of ization F,character Synthesisand A. Dimoglo S, Rollas ShvetsN, REFERENCES T 2 SYNTHESIS NEW HYDRAZONES DERIVATED FROM DERIVATED FROM HYDRAZONES NEW SYNTHESIS Marmara University, Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 81010İstanbul, Türkiye 1-4 . In thisstudy,. In ouraimisto agents. gainofnewactive 1 Gaziantep University, Faculty ofArtsandSciences, DepartmentofChemistry, 27310Gaziantep, Türkiye a poete icuig niatra, anticancer, antibacterial, including properties cal pharmacologi- of range wide a shows and oxime as bases schiff of class special a is hydrazone he -Subtituted phenacyl-1,3,4-oxadiazole-2-thiol phenacyl-1,3,4-oxadiazole-2-thiol S-Subtituted Yusuf SICAK International Symposium onDrugResearch &Development 2011 1 Oruç , EmineElçin ORUÇEMRE E, Unsalan S, Kandemirli Kandemirli S, Unsalan E, BediaKOÇYİĞİT KAYMAKÇIOĞLU ESTER HYDROCHLORIDE HYDROCHLORIDE ESTER {-2 (4-substi- N-{1-[2- *[email protected] DRD 2011 P-018 72 - - - R 4. 3. are screened. mental analysis. Antimicrobial activities of these compounds illuminated by using UV, IR, UV, using by illuminated been have derivatives hydrazide-hydrazones synthesized new the of structure The monohydrate. hydrazine and ves derivati- tedphenyl)carbonyl]amino}-3-sulfanylpropanoate 1 , Ayşegül KARAKÜÇÜKİYİDOĞAN oyğtKyaçol B, Koçyiğit-Kaymakçıoğlu S, Dangre V, Kumar K, Bothara T, Chitre V, Raparti 44: 3954-3960,2009. Chem Med J Eur investigations. QSAR activity bacterial antimyco Synthesis, 4-yl)-N’-(arylidene)benzohydrazide: 4-(morpholin- Novel B. Deshmane S, Gore C, Khachane rivatives. Bioorg Chem16:1822-1831, 2008. Med 286, 2009. from 277- 18: hydrazide”. Res acid 4-fluorobenzoicChem derivedMed hydrazones of activity Antituberculosis O C N H 2 H C L -CYSTEIN ETHYL ETHYL -CYSTEIN C O C H 1 H NMR spectroscopy and ele and spectroscopy NMR H Oruç 2 N H SH E Usln , ols S. Rollas S, Unsalan EE, N C H 1,* , R 1 - - POSTER PRESENTATIONS - C NMR, C 13 H NMR, H 1 thesis and evaluation of anti-HIV activity of isatin Chem Med Bioorg derivatives. β-thiosemicarbazone 15, 4451-4455, 2005. Lett CS., Faria AR., Araujo JM., Lima JG., Alves A., Melo E., Goes A. Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl- 3-thiosemicarbazones and 2-[(phenylmethylene) ac hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic ids. Bioorg Med Chem 16, 446-456, 2008. Bioorg ids. In the present work, we have synthesized twelve thi- twelve synthesized have we work, present the In Bal TR., Anand B., Yogeeswari P., Sriram D. - Syn Aquino TM., Liesen Aquino A., Silva REA., CarvalhoVT., Lima Emine Elçin ORUÇ EMRE ORUÇ , Emine Elçin , Özgül GÜNER * 5. 4. osemicarbazone osemicarbazone derivatives bearing aromatic ring. All sol- appropriate used TLC by monitored were reactions thiosemicarba- of structures chemical The system. vent FTIR, UV-vis, by identified were zones MS spectral data and their purities were determined by by determined were purities their and data spectral MS TLC, melting point and elemental analyses. Their - anti microbial, cytotoxic and antiviral activities are - evalu studies. in future ated - - 73 ' P-019 R DRD 2011 DRD * [email protected] in vitro against s t n e u t i t s N b . Biological activities of thi- u 1 THIOSEMICARBAZONE DERIVATIVES s H N

s o S ri International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International a v

H N =

' R Mycobacterium Mycobacterium tuberculosis was reported

R . The other biological activities of thiosemicar SYNTHESIS AND CHARACTERIZATION OF NOVEL AROMATIC 2

hiosemicarbazones hiosemicarbazones are obtained by - condensa tion of the corresponding thiosemicarbazide with aldehydes or ketones

. Gaziantep University, Faculty of Arts and Sciences, Department of Chemistry, 27310 Gaziantep, Türkiye Türkiye 27310 Gaziantep, Department of Chemistry, of Arts and Sciences, Faculty University, Gaziantep 3-5 R

Ayşegül KARAKÜÇÜK İYİDOĞAN KARAKÜÇÜK Ayşegül Bilal AYDINÖZ, T Trıapıne Trıapıne (3-aminopyridine-2-carboxaldehyde thiosemicarbazone; 3-AP): An of inhibitor ribonucleotide reductase with antineoplastıc activity. Advance En- zyme Regulation 39, 3-12, 1999. a new class of compounds effective tubercle bacilli. Naturwissenschaftentubercle 10, 315, 1946. GY., GY., Campos RH., Cavallaro LV., Moglioni AG. New 1-indanone thiosemicarbazone derivatives active 2008. Med1767-1773, J 43, Chem Eur BVDV. against REFERENCES Finch Finch RA., Liu MC., Cory AH., Cory JG., Sartorelli AC. Domagk G., Behnisch R., Mietzch Schmidt F., H. On Finkielsztein Finkielsztein LM., Castro EF., Fabian LE., Moltrasio 3. 2. 1. bazone bazone derivatives such as antimicrobial, antiprotozoal, anticonvulsant, antiviral and antitumor activity have been de scribed osemicarbazones osemicarbazones have been studied since 1946, when their activity against by Domagk POSTER PRESENTATIONS vulsant, anticancer andantiviral activities anticonantituberculosis,- antimicrobial, as such activites cal hydrazones are also compounds which posses great biologi- NMR, 3. 2. 1. turescompoundsthese of have confirmedbybeen UV, struc chemical and purities future.The in activities ticancer haverealisedtoinvestigatebeen antimicrobialan- their and center chiral a have which hydrazide acid phenyl]propanoic substitutedbenzamido)-N’-(4-substitutedbenzylidene)-3- H ewly K. AdlAi, M, ahn, E. Hussei- MES., Lashine, LM., Abdel-Aziz, KA., Metwally, M., Pufky,Ciesielski, D., Döring, M. A convenient new syn- studies spectral ESR and electronic VP.Synthesis, Singh 4-carboxylic acid hydrazides:Synthesis and preliminary preliminary and hydrazides:Synthesis acid 4-carboxylic 2-aryl-quinoline- of Hydrazones RH. Badawya, MI., nyb, 5942–5947, 2005. dichloride. copper Tetrahedronhydrazonesusing clic 61, heterocy of oxidation the 1,2,4-triazoles: fused of thesis 2008. 17–22, 71, A Part Acta Chim hydrazones. and Spect zines acylhydra- some with complexes nitrate copper(II) on REFERENCES n hs td, ytei o egt (S)-2-[(4- eight of synthesis study, this In SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SOME NEW HYDRAZIDE- NEW SOME OF ACTIVITIES BIOLOGICAL AND SYNTHESIS 13 C NMR,MSspectroscopies andelemental analysis. Gaziantep University, Faculty ofArtsandSciences, DepartmentofChemistry, 27310Gaziantep, Türkiye and preparation of cyclic rings cyclic of preparation and complexesmetal for ligands as synhesis, drug for compounds important of class a are ydrazones International Symposium onDrugResearch &Development 2011 Şenel TEKE,Ayşegül KARAKÜÇÜKİYİDOĞAN HYDRAZONE DERIVATIVES DERIVATIVES HYDRAZONE 3-5 1-2 . . The hydrazide- The . *[email protected]

DRD 2011 IR, P-020 1 H 74 - - 5. 4. Kaushik, D., SA., Chawla, Kumar,Kaushik, G., Khan, S. N’-[(5-chloro- - Kan S., Unsalan, E., Oruç B., Koçyiğit-Kaymakçıoğlu, ity. Eur Chem45,3943-3949,2010. JMed activ anticonvulsant and Synthesis hydrazides: stituted 2/4-sub 3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] Chem41,1253–1261,2006. Med J Eur activity. structure–antituberculosis their of study the and hydrazide–hydrazonesnovel of characterization demirli, F., Shvets, N., Rollas, S., Anatholy, D. Synthesis and 8675–8682, 2006. evaluation as antimicrobial agents. Bioorg Med Chem 14, O R N O H * N H N R ' - - POSTER PRESENTATIONS - - , -(4- 1,* N 2 , Mehmet ÖZASLAN 2 In this study, N-(4-acetylphenyl)-3-nitrobenzamide which N-(4-acetylphenyl)-3-nitrobenzamide study, this In ap R. Synthesis and antihyperglycemic activity of chalcone based aryloxypropanolamines. Bioorg Med Chem 12: 883-889, 2004. Shanker K, Chanotiya CS, Gupta MM, Negi AS. Sythesis of chalcone derivaties on steroidal framework and their an- 72: 892-900, 2007. activities. Steroids ticancer Satyanarayana M, Tiwari P, Tripathi BK, Srivastava AK, Prat AK, Srivastava BK, Tripathi P, Tiwari M, Satyanarayana Saxena Saxena HO, Faridi U, Kumar JK, Luqman S, Darokar MP, Ayşegül KARAKÜÇÜK İYİDOĞAN , Ayşegül 1 were reacted with 4-aminoacetophenone and 3-nitrobenzoil 3-nitrobenzoil and 4-aminoacetophenone with reacted were chloride and then this compound were treated with suit able substitue aldehydes in order to obtain new N-(4-{3-[4- substituephenyl]prop-2-enoyl}phenyl)-3-nitrobenzamide derivatives. The structures of synthesized compounds were identified from appropriate. The structures of synthesized and NMR 1H NMR, 13C IR, UV, by identified were compounds elemental analysis (C, H, N, S). All compounds were - evau lated for antimicrobacterial activity against Gram-pozitive (Pseudomonas aeruginosa ATCC 25853, 25322) Escherichia ATCC ve Gram-negative (Enterococcus faecalis ATCC coli 29212) with 25923, microdilution Stafilococcus aureus ATCC process. broth 4. 5. - - - - 75 P-021 DRD 2011 DRD Derya İŞLER , Derya 2 *[email protected] CHARACTERIZATION literature literature studies, a wide range of phar show show Emine Elçin ORUÇ EMRE , Emine Elçin 1 İbrahim Halil KILIÇ İbrahim

International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International . 1-5 the chalcones

Erdem ERGAN Erdem halcones halcones are 1,3-diphenyl-2-propene-1-one, in which two aromatic rings are linked by a three carbon α,β-unsaturated carbonyl system. Chal- Gaziantep University, Faculty of Arts and Sciences, Department of Biology, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Biology, of Arts and Sciences, Faculty University, Gaziantep 2 Gaziantep University, Faculty of Arts and Sciences, Department of Chemistry, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Chemistry, of Arts and Sciences, Faculty University, Gaziantep THE SYNTHESIS OF NOVEL CHALCONE DERIVATIVES FROM

ACETYLPHENYL)-3-NITROBENZAMIDE AND THEIR STRUCTURAL 1 P, Khan SR. Anticancer activities of novel chalcone and bis- and chalcone of novel activities Anticancer SR. Khan P, 2006. 3491-3495, 14: Chem Med Bioorg derivaties. chalcone CN. Synthesis and biological evaulation of simple methox simple of evaulation biological and Synthesis CN. ventive agents. Bioorg Med 16: 7270-7276, 2008. Chem Bioorg agents. ventive an and anti-inflammatory as anticancer, chalcones ylated 2010. 1364-1370, 18: Chem Med Bioorg agents. tioxidant thesis and cytotoxic, anti-inflamatory, and anti-oxidant as chemopre cancer activities of 2’,5’-dialkoxylchalcones REFERENCES Modzelewska A, C, G, NE, Pettit Achanta Huang Modzelewska Davidson Bandgar BP, Gawande SS, Bodade RG, Totre JV, Khobragade Khobragade JV, Totre RG, Bodade SS, Gawande BP, Bandgar

- Syn CN. Lin SJ, Won JP, Wang SC, Yang CF, Hung JH, Cheng C

cones cones possess conjugated double bonds and a completely delocalized π-electron system on both benzene rings. Chal- cones are synthesized by Claisen-Schmidt condensation of aldehyde and ketone by base catalyzed or acid catalyzed by followed Indehydration. the result of macological macological properties including antibacterial, anticancer, antifungal, antiinflammatory, antitubercular, antitrombosit, antimalarial, antiparasitic, antidiabetic, antileishmanial, an- activitiestiplatelet it is known that 2. 3. 1. POSTER PRESENTATIONS rial, antimycobacterial, antimycotic, antifungal and anti-inflammatory panoate have been synthesized. been have panoate fromderivated 1,3,4-tiadiazoles cent studies 3. 2. 1. sant and antiviral and sant in drugs. N 1,2,4-TRIAZOLE-3-THIONES AND 1,3,4-THIADIAZOLES DERIVED FROM FROM DERIVED 1,3,4-THIADIAZOLES AND 1,2,4-TRIAZOLE-3-THIONES Kritsanida Kritsanida M, Mouroutsou A, Marakos P, Pouli N, Papakon - MG, Mamolo Falagiani V, Zanpier D, Vio L, Banfi F. Synthe VarvarasonA, Tantili-KakoulidouSiatra-PapastasikoudiA, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITIY OF NEW NEW OF ACTIVITIY BIOLOGICAL AND CHARACTERIZATION SYNTHESIS, n hs td, oe oe 124tizl--hoe and 1,2,4-triazole-3-thiones novel some study, this In stantinou-Garoufalias S, Pannecouque C, Witvouw M, De De M, PannecouqueC, Witvouw S, stantinou-Garoufalias rivatives. Farmaco 56:587-592,2001. de arylidene-hydrazide acid thiadiazol-2-yl-thio)]-acetic 5-(pyridin-2-1,3,4- of activity antimycobacterial and sis Forsch 50:48-54,2000. Arzneim analogs. 1,3,4-thiadiazole and 1,2,4-triazole clic containing derivatives of thiosemicarbazide and their cy T, Tiligada E. Synthesis and biological evaluation of indole REFERENCES Gaziantep University, Faculty ofArtsandSciences, DepartmentofChemistry, 27310Gaziantep, Türkiye The ring the structure of many organic compounds used compounds organic many of structure the occur that 1,3,4-thiadiazole and 1,2,4-triazole as such rings heterocyclic owadays,five-membered has established for these heterocycles analgesic 3 systems , biological 5 activities. International Symposium onDrugResearch &Development 2011 of the ETHYL-2-AMINO-3-PHENYLPROPANOATE

activity Eyüp BAŞARAN,Ayşegül KARAKÜÇÜKİYİDOĞAN* activity ethyl-2-amino-3-phenylpro Chemical structure of the of structure Chemical

was observed. was

studies 1,2 on antibacte , anticonvul- *[email protected] Even re- Even DRD 2011 P-022 76 - - - - - 4

NMR, synthesized compounds were elucidated with UV-vis, IR, UV-vis, with elucidated were compounds synthesized compounds willbescreened these of anticonvulsant timicrobial,activities and anticancer 5. 4. R Labanauskas Labanauskas L, Kalcas V, Uderenaite E, Gaidelis P, Brukstus G, FalconeW, Bondavalli A, Ranise O, Bruno S, Shenone matory activity.matory Pharmazie 56:617-619,2001. anti-inflam- exhibiting derivatives )-1,3,4-thiadiazole nyl 2-amino-5-(3,4-dimethoxyphe and 1,2,4-triazole-5-thiol 3-(3,4-dimethoxyphenyl)-1H- of Synthesis V. Dauksas A, agents. Bioorg Chem9:2149-2153,2001. Med analgesic and anti-inflammatory as thiadiazol-2(3H)ones Arylsulphonyl-5-arylamino-1,3,4- M,3- Vitelli L, Giordano Clercq Farmaco E. Il 57:253–257,2002. O 13 C NMR, MS spectral data and elemental analysis. An- analysis. elemental and data spectral MS NMR, C N H N S N N H R . 1 R O H N N N H S N 1 R H - 1 POSTER PRESENTATIONS - - S. , 1 S. aureus 6538, ATCC C NMR, MS spectrosco 13 Mehmet SÖNMEZ , Mehmet 1 H NMR, 1 2 IR,

M. luteus 9345) ATCC was investigated , Demet TAŞDEMİR In vitro antibacterial activity of thiosemicarbazones and , İsmet BERBER 1 The The puritiy and chemical structure of the ligands were Krettli AU., Krettli Zani AU., CL. Synthesis and antimalarial activity of semicarbazone and thiosemicarbazone derivatives. Eur J Med Chem 43: 1983-1988, 2008. thesis and antimycobacterial activity of new S-alkyliso thiosemicarbazone derivatives. Bioorg Med Chem 10: 501–506, 2002. Oliveira R., Souza-Fagundes E.M., Soares RP., Andrade AA., Andrade RP., Soares E.M., Souza-Fagundes R., Oliveira Cocco A., Cenzo Congiu C., Onnis V., Pellerano M. - Syn 1,* determined determined by UV-vis, pies and elemental analysis. Their complexes with Ni(II), Zn(II) Cu(II), and Co(II) were proposed from combination of UV-Vis, IR, MS spectra, elemental analysis and TGA. These studies revealed that thionic sulphur and azomethine nitrogen of thiosemicarbazones were coordinated to metal ion. their complexes against bacteria Gram-negative and Gram- positive bacteria (E. coli 4230, ATCC 3. 4. by by microdilution broth method. Ampicillin was used as the standart for antibacterial test and the minimum inhibitory determined. (MIC)were compounds these of concentrations ATCC aureus ATCC 25923, - - - - 77 P-023 and DRD 2011 DRD 3 ' R R *[email protected] THIOSEMICARBAZONES , antimalarial 2 N H N S

Emine Elçin ORUÇ EMRE Emine Elçin N H N H M S N N H International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International , antineoplastic 1 Ayşegül KARAKÜÇÜK İYİDOĞAN KARAKÜÇÜK , Ayşegül 1 ANTIBACTERIAL ACTIVITY OF SOME NEW AROMATIC

. In this we have study, syntesized Cu(II), Ni(II), Sinop Unıversity, Faculty of Arts and Sciences, Department of Biology, 57000 Sinop, Türkiye of Biology, Department of Arts and Sciences, Faculty Sinop Unıversity, 2 ' 4 R

R hiosemicarbazones hiosemicarbazones are universal ligands because they can as coordinate neutral ligands or their de protonated forms so these group crucial for coor Gaziantep University, Faculty of Arts and Sciences, Department of Chemistry, 27310 Gaziantep, Türkiye 27310 Gaziantep, Department of Chemistry, of Arts and Sciences, Faculty University, Gaziantep 1

Bilal AYDINÖZ T

LN., Rath N., Padhye S. Appended 1,2-naphthoquinones as anticancer agents 1:synthesis, structural, spectral and antitumor activities of ortho-naphthaquinone emicarbazone and its transition metal complexes. thios- Inorg Chim Acta 357: 271–278, 2004. REFERENCES oxy-1,2-bis(thiosemicarbazone) derived from D-glucose. Res 328: 425-429, 2000. Carbohyd

Horton D., Varela O. Cu, Pt, and Pd complexes of the 3-dethe of complexes Pd and Pt, Cu, O. Varela HortonD., Zakharov AL., Rheingold Y., Ma J., Che, E., Sinn Z., Afrasiabi Zn(II), Co(II) complexes of thiosemicarbazone derivated from from derivated thiosemicarbazone of complexes Co(II) Zn(II), 4-substitutedbenzaldehydes and N-phenylhyhidrazinecar bothioamide. bothioamide. 1. 2. antimicrobial dination dination chemistry .Thiosemicarbazones coordinate to the metal ion by the sulphur and nitrogen atoms. Consequently recently thiosemicarbazones and their metal complexes are considerable interest. They have been important biological activity such as antiviral

POSTER PRESENTATIONS larial such as antituberculosis activities, pharmacological of range wide a have complexes palladium and platinum their and derivatives emicarbazone hyhidrazinecarbothioamide. and 5-substitutedthiophene-2-carboxaldehydes from derivated thiosemicarbazone of complexes Pd(II) and Pt(II) syntesized have we study, this In compounds. these in tivity of ribonucleotide reductase ribonucleotide of tivity the ac to blocking by cells L1210 leukemia in DNA of biosynthesis inhibit CT) Haven, New Inc. Pharmaceuticals Vion (Triapine®; thiosemicarbazone nopyridine-2-carboxaldeyde 3-ami- evample, For cells. cancer of activities the inhibiting for useful potentially agents chemotherapeutic as proved 3. 2. 1. R 2 Laboratory ofVirology andChemotherapy, RegaInstitute for Medical Research, Katholieke Universtiteit Leuven, aío E, uaGls . Grí P, adrn . Co(III), M. Calderón P., García F., Luna-Giles E., Zahínos VasquezR., Loomis SP.,WC., Gril Rose MC., Liu RA., Finch 46: 150-159,2011. Chem Med J Eur activity. antibacterial and structures ray X- characterization, Synthesis, thiosemicarbazone: line 2-acetyl-2-thiazo with complexes Cd(II) and Zn(II) Ni(II), wirksame vitro 10:315,1946. Verbindungsklasse. Naturwis-senschaften in Tuberkelbazillen gegen neue eine Uber Schmidt. H. F.Mietzsch., Behnisch., R. Domagk., G. antitumor activity. spectrum broad with activity reductase ribonucleotide of inhibitor potent a 2-carboxaldehyde-thiosemicarbazone): AC. Sartorelli YC.,Cheng KM., REFERENCES Demet TAŞDEMİR 5 , antiviral , PALLADIUM(II) COMPLEXES DERIVED FROM 5-SUBSTITUTED-2- FROM DERIVED COMPLEXES PALLADIUM(II) lcto i pamcuia ceity n have and chemistry pharmaceutical in plication ap their to due importance achieved have plexes com - metal their and thiosemicarbazones ecently, ANTIVIRAL AND CYTOTOXIC ACTIVITIES OF PLATINUM(II) AND AND PLATINUM(II) OF ACTIVITIES CYTOTOXIC AND ANTIVIRAL 1 Gaziantep University, Faculty ofScience, DepartmentofChemistry, 27310Gaziantep, Türkiye THIOPHENE CARBOXALDEHYDE THIOSEMICARBAZONES CARBOXALDEHYDE THIOPHENE 6 so that many research groups are interestedareresearchgroupsmany that so Biochem Pharmacol 2 , antimicrobial 1 International Symposium onDrugResearch &Development 2011 , Ayşegül KARAKÜÇÜKİYİDOĞAN Triapine (3-aminopyridine- Triapine 1 . Many heterocyclic thios- heterocyclic Many . 3 , antitumor 59: 983-991, 2000. * [email protected] 3000 Leuven, Belgium N-phenyl- 4 , antima- DRD 2011 P-024 78 - - - 6. 5. 4. n atvrl ciiy f l tismcraoe ad their and metal complexes were alsoevaluated. thiosemicarbazones all of activity antiviral and The ion. metal to coordinated were zones - thiosemicarba that of nitrogen azomethine and sulphur revealedthionic studies These TGA. and analysis elemental spectra, MS IR, UV-Vis, of combination from proposed were pies and elemental analysis. Their complexes with Pt(II), Pd(II) determined by UV-vis, by determined 1,* Quenelle D., Keith K., Kern E. In vitro and in vivo evalu - vivo in and vitro In E. Kern K., Keith D., Quenelle Walcourt A., Loyevsky M., Lovejoy D., Gordeuk V., Richard- antitu- and Synthesis J. Ren H., Xu S., Pan YangZ., K., Hu 71, 24-30,2006. Research Antiviral infections. virus cowpox and vaccinia against marboran and isatin-thiosemicarbazone of ation Biol 36:401–407,2004. resistant and -sensitive parasites. The Int J Biochem & Cell chloroquine- against activity anti-malarial with chelators son R. Novel aroylhydrazone and thiosemicarbazone iron tives. Eur Chem45:3453-3458,2010. JMed deriva- thiosemicarbazone liquiritigenin of activity mor h prty n ceia srcue f h lgns were ligands the of structure chemical and puritiy The R , EmineElçin ORUÇEMRE M=Pt(II) Pd(II)or N H

IR, S 1 H NMR, H Cl N M N 1 13 , JanBALZARINI C NMR, MS spectrosco MS NMR, C Cl cytotoxic vitro in S R ' 2 - POSTER PRESENTATIONS - - - H- 1 . 5,6 to find more International th (II)

l C H

. N -position with chlorine atom. atom. chlorine with -position 1 N p ) R I O I ( C O 2 ) 3 This project was supported by Hacette by supported was project This CH(CH l 2 C -imidazole-1-yl)ethanol esters esters -imidazole-1-yl)ethanol International Symposium on Pharmaceutical Pharmaceutical on Symposium International H H th O , -CH 3 O C - Sevim DALKARA , Sevim CH with various aliphatic carboxylic acids in the presence presence the in acids carboxylic aliphatic various with R 2 ) 1, * 2 (I) (CH N Chemistry (ISPC) Septem- Joint Meeting, Ankara-Türkiye, ber 30-October 90, 2010. 2, 2010, Abstract Book p. In this study we aimed to synthesize some In new 1-(4-chlo we this study to aimed synthesize Meeting on Medicinal and Pharmaceutical (IMMPC)-6 Chemistry Acknowledgement: tives tives of 1-(2-naphthyl)-2-(1,2,4-triazol-1-yl)ethanone and their anticonvulsant and antimicrobial activities. Arch. (Weinheim)Pharm. 339: 513-520, 2006. anticonvulsant and antimicrobial activities of some new 2-acetylnaphthalene derivatives. Bioorg & Med Chem 18(8): 2902-2911 (2010). H-imidazol-1-yl) 1-phenyl-2-(1 ethanol. 4 Karakurt A, Özalp M, Işık Ş, Stables JP, Dalkara S. Synthesis, Synthesis, S. Dalkara JP, Stables Ş, Işık M, Özalp KarakurtA, of esters aliphatic on Studies S. Dalkara S, Saraç İS, Doğan 2 N of dicyclohexylcarbodiimide/4-dimethylaminopyridine IR, (DCC/ by of confirmed was dicyclohexylcarbodiimide/4-dimethylaminopyridine compounds the of structure The DMAP). active and less toxic anticonvulsant and antifungal compounds compounds antifungal and anticonvulsant toxic less and active compounds In these group. this for SARs new to and establish at substituted was ring phenyl the appropriate of the esterification by prepared were Compounds alcohol rophenyl)- 2-(1 rophenyl)- NMR, mass spectral data and elemental analysis. analysis. elemental and data spectral mass NMR, 010D06301004). (HÜBAB Fund Research Scientific University pe and aliphatic carboxylic and acid carboxylic aliphatic of ester derivatives 1-phenyl-2- aro ring as a phenyl lipophilic carrying (imidazol-1-yl)ethanol described been have naphthalene of instead group matic 5. 6. , -CH ) 3 H I . ------( O 79 1,2 CH 2 P-025 DRD 2011 DRD -azole -azole CH 2 H , Selma SARAÇ l Türkiye Çünür-Isparta, -imidazole- C 1, 2 , -CH [email protected] H 3 * . In our previ our In . 4 3,4 H CH B 2 36: 421-433, 2001. 421-433, 36: a

N , -CH 3 N N R: -CH O Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06100 Ankara, Türkiye Ankara, 06100 Chemistry, Department of Pharmaceutical of Pharmacy, Faculty

İnci Selin DOĞAN International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International examples examples of anticon (arylalkyl)azole

-IMIDAZOLE-1-YL)ETHANOL ESTERS AS POTENTIAL H l ANTICONVULSANT AND ANTIFUNGAL COMPOUNDS C 2-(1 show antifungal and/or antibacterial activities be activities antibacterial and/or antifungal show

1-ethanol), nafimidone [1-(2-naphthyl)-2-(imidazol- nafimidone 1-ethanol), nafimidone metabolite major its and 1-yl)ethanone] enzimol (α-[4-(2-phenylethyl)phenyl]-1 enzimol

Hacettepe University, Hacettepe 1 imidazole imidazole derivatives, a new class of anticonvulsant agents. J Med Chem 24: 67-74, 1981. REFERENCES Synthesis of some 1-(2-naphthyl)-2-(imidazole-1-yl)ethanone of 1-(2-naphthyl)-2-(imidazole-1-yl)ethanone some Synthesis anticonvulsant and their derivatives ether Chem and oxime oxime Med J Eur activities. antimicrobial and tivity of N-(benzoylalkyl)imidazoles and N-(ω-phenyl-ω- J Med Chem 24: 727-731, 1981. hydroxyalkyl)imidazoles. istretti istretti MJ, Subissi A. Synthesis and anticonvulsant ac Özbey S, Dalkara S. Synthesis of some oxime ether deriva- ether oxime some of Synthesis S. Dalkara S, Özbey Walker Walker KAM, Wallach MB, Hirschfield DR, H- 1-(Naphthylalkyl)-1 Karakurt A, Dalkara S, Özalp M, Özbey S, Kendi E, Stables JP. JP. E, Stables S, Kendi M, Özbey S, Özalp A, Dalkara Karakurt Nardi Nardi D, Tajana A, Leonardi A, Pennini R, Portioli Mag- F, Karakurt A, Aytemir MD, Stables Özalp JP, M, Kaynak FB, SYNTHESIS AND CHARACTERIZATION OF NEW 1-(4-CHLOROPHENYL)- Permanent address: Süleyman Demirel University, Faculty of Medicine, Research and Implementation Hospital, Hospital, and Implementation Research of Medicine, Faculty University, Demirel Süleyman address: Permanent

2 D

3. 2. 1. alcohol alcohol are known the vulsant compounds. The structure-activity relationship (SAR) relationship The vulsant compounds. structure-activity activ that showed the anticonvulsant studies most desirable ity with appeared a aryl lipophilic oxygen group, containing ring and in bridge imidazole the alkylene substituent small pounds also pounds cause to of 1-substituted-1 similarities their structural fluconazole and itraconazole) as an azole group azole an as itraconazole) and fluconazole In addition to their anticonvulsant activity, many of these com these of many activity, anticonvulsant their to addition In the among other place an have which important antifungals, an possess generally antifungals Azole compounds. antifungal ketoconazole, miconazole, with (seen ring triazole or imidazole ous studies some carboxylic acid esters of nafimidone alcohol alcohol of nafimidone esters acid carboxylic some studies ous 4. POSTER PRESENTATIONS acid significantly decreased following the administration of the of administration the following decreased significantly were behaviors stretching and writhing acid-induced acetic of numbers and increased significantly were tests tail-clip and hot-plate in mice of times Reaction compounds. the test by induced abnormalities motor any of presence the check to werereferenceperformed tests a Rota-roddrug. as used was mg/kg) (10 sulphate Morphine mice. in tests ing - writh induced acid acetic and tail-clip plate, hot by gated investi- were mg/kg) (100 compounds test the of activities Antinociceptive Analyses. Elemental and and data roscopic 1. rvd y en o ter IR, their of means by proved SYNTHESIS AND ANTINOCICEPTIVE ACTIVITY OF SOME 2-PYRAZOLINE 2-PYRAZOLINE SOME OF ACTIVITY ANTINOCICEPTIVE AND SYNTHESIS Srinath N., Prasad Y.R., SynthesisK., and Mukkanti analge J Curr 3(1),76-80,2010. Pharm Res 1,3,5-trisubstituted-2-pyrazolines,Int some of activity sic REFERENCES T 1 1 Te tutrs f h snhszd opud were compounds synthesized the of structures The . Anadolu University, Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 26470Eskişehir, Türkiye Ahmet ÖZDEMIR oe wt hdaie yrt i gail acetic glacial in hydrate hydrazine with cones chal- various reacting by synthesized were tives deriva- 1,3,5-trisubstituted-2-pyrazoline new he 3 AnadoluUniversity, Faculty ofPharmacy, DepartmentofPharmacology, 26470Eskişehir, Türkiye International Symposium onDrugResearch &Development 2011 2 Anadolu University, Faculty ofPharmacy, 26470,Eskişehir, Türkiye 1,* , EbruÇINAR 1 -M ad FAB and H-NMR GülhanTuran ZITOUNI 2 , MehlikaDilek ALTINTOP + * M spect -MS [email protected] DERIVATIVES DERIVATIVES DRD 2011 P-026 80 - - 1 needed to clarify the exact mechanismofaction. needed to theexact clarify both peripheral and central mechanisms. Further studies are antinociceptive activities and these antinociception involves of levels different exhibited compounds tested conclusion, In abnormalities. motor to due occurred unlikely ciception mance in Rota-Rod test, indicating that the observed antino perfor motor the impair not did compounds The activity. antinociceptivepresenceof compounds,the testindicating R , ÖzgürDevrim CAN =

- C H 2 - O - C H 2 ,

- OC 2 H 1 5 , , Zafer AsımKAPLANCIKLI

- N S ( C 2 O H 5 ) N 2 , 3

- OH, N

- C H ( C H 3 ) 2 ,

- C R N,

- C F 3 ,

-Br ,

- C H 1 , 3 ,

- OC F 3 - - POSTER PRESENTATIONS - - - , 2 asu -B This This study was supported by Sci- 2 aushik K , Neerja 1,* In view of the above observations, the green synthesis Acknowledgement: of some 1-(4-chlorophenyl)-4-hydroxy-1H-pyrazol-3-car bonyl bonyl derivatives linked to nitrogenous heterocyclic ring Chem Med Bioorg agents. antitumor potential as systems 18, 2767-2776, 2010. K, Watashi Shimotohno K, Baba M. Anti-bovine viral diar rhoea virus and hepatitis C virus activity of the cyclooxy genase inhibitor SC-560. Antivir Chem Chemother 20 (1): 47-54, 2009. Rostom SAF. Rostom Polysubstituted pyrazoles, SAF. part 6. Synthesis Okamoto M, Sakai M, Goto Salim Y, MT, Baba C, Goto K, proved to be a selective inhibitor of HCV replication [5]. of HCV be a selective inhibitor to replication proved of novel 1-aroyl-3,5-dimethyl-1H-pyrazole derivatives using biological investigating at aimed were irradiation microwave activities of these compounds. entific Research Project Commission of Marmara University / 0175). number: SAĞ.A.310510 (Project 4. 5. ydın - - 81 A Türkiye P-027 DRD 2011 DRD Newark, NJ 07103 Newark, were were re Sevil , Sevil 1 [email protected] * SOME HYDRAZIDES Guru Kumar Kollongod RAMANATHAN Guru Kumar Kollongod üçükgüzel K neovascularization, neovascularization, decrease

International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Ş.Güniz Ş.Güniz

in VEGF production and increase in apoptosis of yrazole-containing compounds ported to exhibit

Facile Facile synthesis and in-vitro antitumor activity of some pyrazolo[3,4-b]pyridines and pyrazolo[1,5-a]pyrimidines linked to a thiazolo[3,2-a]benzimidazole moiety. Arch Sci 342: 230-237, 2009. Chem Life Pharm substituted substituted pyrazole derivatives and their evaluation as antitumor and antiangiogenic agents. Chem Pharm Bull 51(7): 838-844, 2003. (Tokyo) in Angiogenesis. Curr Med Chem 7: 1163-1170, 2000. Curr in Angiogenesis. REFERENCES Abdel-Aziz HA, Gamal-Eldeen AM, Hamdy NA, Fakhr IMI. Abadi AH, Eissa AA, Hassan GS. Synthesis of novel 1,3,4-tri- novel of Synthesis GS. Hassan AA, Eissa AH, Abadi Leahy KM, Koki AT, Masferrer JL. Masferrer Role of Cyclooxygenases KM, KokiLeahy AT,

Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, İstanbul, Haydarpaşa 34668 Chemistry, of Pharmaceutical Department of Pharmacy, Faculty University, Marmara P 1 SYNTHESIS AND CHARACTERIZATION OF PYRAZOLE DERIVATIVES FROM Department of Biochemistry and Molecular Biology, UMDNJ-New Jersey Medical School, 185 South Orange Avenue, Avenue, School, 185 South Orange Medical Jersey UMDNJ-New Biology, and Molecular Department of Biochemistry 2 3. 2. 1. tumor cells and antiproliferative activity [1-4]. Pyrazofurin; the natural 4-hydroxypyrazole C-glycoside has antimicro bial and antiviral activities against many RNA and DNA viruses. In addition, this drug has been used clinically as an anticancer agent. 5-(4-Chlorophenyl)-1-(4-methoxyphenyl)- 3-(trifluoromethyl)-1H-pyrazole (SC-560) was reported to be active against bovine viral diarrhoea virus (BVDV) and POSTER PRESENTATIONS phase ACE C ACE phase reversed- on out carried was Separation study. this in used UV detector with a thermostatted column compartment was wavelength variable a and autosampler, pump, quaternary An Agilent 1200 series HPLC system, consisting of a degasser, internal standard (IS) was obtained from Sigma-Aldrich (USA). as used Acetaminophen Turkey). (Ankara, Industry ceutical 2. teoarthritis os- and arthritis rheumatoid of symptoms and signs the for and analgesia of treatment the for indicated is well-tolerated and NSAID, and effective an is acid) b]-indole-1-acetic Etodolaceffect1. ic (1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4- ture of acetonitrile-water (80:20, v/v). The UV detector was detector UV The v/v). (80:20, acetonitrile-water of ture 1. N Zaher A. R, Nasir K. Khan. Effects of cyclooxygenase inhi- cyclooxygenase of Effects Khan. K. Nasir R, A. Zaher tdlc a knl sple fo Nvgnx Pharma- Novagenix from supplied kindly was Etodolac sicologic Pathalogy 58:163-173,2006. gastrointestinaltract.Experimentaland the on Tokbition REFERENCES Department ofAnalytical Chemistry, Faculty ofPharmacy, Atatürk University, 25240Erzurum,Türkiye their anti-inflammatory, analgesic and anti-pyret todue animals aredomestic and humans in used (NSAIDs) drugs anti-inflammatory on-steroidal D 18 etermination column. The mobile phase contained a mix a contained phase mobile The column. International Symposium onDrugResearch &Development 2011 Alptuğ ATİLA, Ö.Faruk KOÇAK, Yücel KADIOĞLU P harmaceutical

with HPLC-UV M HPLC-UV DRD 2011 P-028 82 - - - 2. low cost ofanalyse. and analysis short of because laboratories control quality and concentration. This method can be applicable in routine sensitive. There is an excellent correlation between peak area and linear precise, accurate, specific, are methods present The tablets. in etodolac determining in applied be to oped ofthemethod. linearity experiments, y = 1,530x-0,057 (r = 0.9996), demonstrated the replicate six from equation calibration The solution. stock working IS solution (1 µg mL working tion of six-point calibration curve (0.08–10 µg mL (0.08–10 curve calibration six-point of tion was used to prepare the spiking stock solutions for construc solution working Etodolac program. software ChemStation Agilent using integratedwere areas peak and 272 nm at set samples at three different levels (0.1, 4.5, 9.5 µg mL 9.5 4.5, (0.1, levels different three at samples P Joseph P.LyeiteJoseph S., S. K. Donna PatrickM., K.B., M. Joan B., in Patients with Stable Juvenile Rheumatoid Arthritis Arthritis 21:1715-1724, 1999. Rheumatoid Juvenile Stable with Patients in Etodolac of Pharmacokinetics W.,D. Philip R., Robert R., sml ad uc aayia mto hs en devel- been has method analytical quick and simple A reparations ethod

of E todolac −1 ) was prepared by diluting the

−1 ) and QC and ) −1 ). The ). - POSTER PRESENTATIONS - -

were were

2 lıquıd san

A y ) B almeterol , Adem 1 ) is an important physico- a pK anlı Ş C. 0 C DRUGS (S hioridazine ı values is widely used in recent years. Inthis years. recent in used widely is values a T at at different acetonitrile-water mixtures, - rang , Nurullah 1 values of some basic drugs, namely; fluticasone a and

The The ionization constant ( zapine and thioridazine enhance amphetamine-induced 21:97–101, 1984. Biochem Behav Pharmacol stereotypy. Robertson A, MacDonald C, A typical neuroleptics clo aradaş ing between 55-65% (v/v), using RP- LC-UV method. X-Terra 18 column (250 x 4.60 mm ID x 5m) was used and column 25 was temperature chemical parameter of a drug and the knowledge of parameter this is of fundamental importance in a wide range of applications and research areas. The use of high perfor mance liquid chromatography (HPLC) retention parameters pK determine to study, study, pK determined determined propionate, propionate, salmeterol, xinafoic acid and thioridazine 2. K - - 83 Türkiye OF SOME BAS P-029 DRD 2011 DRD Nurgül , Nurgül 1 [email protected] *

propıonate

alues chromatography anlı V Ş a K p of

, Senem 1,2,* International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International lutıcasone , F alçın Y Department of Chemistry, Faculty of Science and Arts, Hitit University, Çorum, Türkiye University, and Arts, Hitit of Science Faculty Department of Chemistry, 1

luticasone propionate is a glucocorticoid with po tent anti-inflammatory activity used in the - preven tion of asthma. It is very poorly water soluble and

Bediha etermination Department of Analytical Chemistry, Faculty of Science and Arts, Ondokuz Mayıs University, Kurupelit, Samsun, Kurupelit, Samsun, Ondokuz Mayıs University, and Arts, of Science Faculty Chemistry, Department of Analytical REFERENCES verse-phase high performance liquid chromatographic method for concurrent assay of a weak base (salmeterol xinafoate) and a pharmacologically active steroid (fluticasone propionate). J Pharm and Biomed Anal 40:1149- 1154, 2006. Murnane D, Martin GP, Marriott C, Validation of a re

2 F D xınafoate 1. also displays a high degree of binding to lung tissue. Sal - meterol xinafoate dissociates in solution to yield salmeterol base and hydroxynaphthoate, and displays poor aqueous solubility. Thioridazine is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia 1,2. and psychosis POSTER PRESENTATIONS tients withasthma. pa- forlife of quality better a provide and symptoms function, reduce lung improve to inhalation via used agonist tor adrenocep β-2 potent long-acting a is Salmeterol steroids. cortico inhaled available other with compared rhinits and asthma of treatment the in efficacy therapeutic improved 2. 1. SALMETEROL XINAFOATE SALMETEROL F 2 Murnane Murnane D, GP,Martin Marriott C, Validation of a RP-HPLC Li YN, TattamBrown,KF,BN, JP,Seale, method sensitive A method for concurrent assay of a weak base (salmeterol base weak a of assay concurrent for method etry. JPharm BiomedAnal 16:447-452,1997. - spectrom mass ionisation chemical pressure mospheric chromatography/at liquid high-performance by plasma for the quantification of fluticasone propionate in human REFERENCES Department ofAnalytical Chemistry, Faculty ofScience andArts,OndokuzMayısUniversity, Kurupelit,Samsun, inflammatory activity. It has been shown to exhibit to shown been has It activity. inflammatory anti- pulmonary potent having cocorticosteroid glu- androstane novel a is propionate luticasone SIMULTANEOUS ASSAY 1 Department ofChemistry, Faculty ofScience andArts,HititUniversity, Çorum,Türkiye Bediha International Symposium onDrugResearch &Development 2011 Y alçın 1,2 , Senem ın * [email protected] P harmaceutical of Ş anlı DRD 2011 FLUTICASONE PROPIONATE AND AND PROPIONATE FLUTICASONE P-030 Türkiye 84 - - - 1,* , Nurullah mM ortophosphoric acid. mM ortophosphoric 25 with 3.75 pH to adjusted (v/) 60:40 acetonitrile:water of ) at 25 at 5m) x ID mm 4.60 x mm (250 on performed was Separation form. dosage pharmaceutical in xinafoate salmeterol and pionate oped for the simultaneous determination of fluticasone pro devel- been have chromatographicmethod liquid validated fully and precise accurate, simple, A formulation1,2,3. bined com - in or individually inhalers meteredpressurizeddose or 3. Zhang M, Fawcett,M, Zhang P, Shaw, JP, chiral HPLC Rapid assay for These two drugs are formulated as dry powder inhalers powder dry as formulated are drugs two These 1999. 729:225-230, B Chromatogr J studies. metabolism vitro in to Application a-hydroxysalmeterol. and salmeterol 2006. 40:1149-1154, Anal Biomed Pharm J propionate). casone (fluti- steroid active pharmacologically a and xinafoate) Ş anlı D osage 1 , Adem F A san 0 orms with C -er R-8 column RP-18X-Terra 2

the mobile phase mobile the B y H plc - POSTER PRESENTATIONS - 5, 5) H 6 3) as C 3 Staphy tropicalis, tropicalis, 5 p-CH 5, H 6 H 6 Candida Candida krusei. Candida 2 J Heterocycl Chem R p-ClC 2,6-Cl C 5, 5, H 6 H 1 6 C : C : R 2 2 N N R 5 1) was shown moderately - anti H 1 6 p-NO C 5, 2 Synthesis, Synthesis, antiviral and - antitu H 6 Candida Candida , albicans C , CH , 2 5 lgül ) 3 H A 6 p-N(CH , p-Cl, C 5, 5 . Bioorg Med Chem 15: 4419-4426, 2007. . Bioorg H H 6 6 Additionally, all compounds were were compounds all Additionally, cereus. Bacillus and C Öztekin , Öztekin 3 2 : C : 1 R mor activity of 2-substituted-5-amidino-benzimidazoles 2(2): 27-34, 2010. Lettre Pharmacia thesis and antimicrobial properties of benzylsulfanyl)-1. h-benzimidazoles 2-(substituted- 42: 1405-1408, 2005. Karminski-Zamola G. Kumar Kumar RV, Gopal KR, Sheshu Kumar KVSR. Facile syn- Starcevic K, Kralj M, Ester K, Sabol I, Grce M, Pavelic K, predominantly predominantly more effective against gram positive than 1,2-diphenyl-1H- hand, other the On bacteria. negative gram benzimidazole (Compound fungal activity against The The most potent antibacterial effective compounds were H-benzimidazole 1,2-bis(4-chlorophenyl)-1 (Compound they were demonstrated most inhibitory effect on lococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and 1-benzyl-2-phenyl-1 H-benzimidazole (Compound 4. 5. p-OCH We We have concluded that substitution at N-1 and C-2 posi- activity was antimicrobial on ring benzimidazole the of tions important and our next studies will be focused on effect of activity. these substitutions on antimicrobial Candida Candida parapsilosis, Candida glabrata and uran - D 85 P-031 DRD 2011 DRD resis - [email protected] * , Nizami 1,* ethicillin J Clin Microbiol arı T NEW BENZIMIDAZOLE DERIVATIVES Özden [1,2]. Drug resistance is also in- International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Mersin University Faculty of Medicine Department of Microbiology, Hatay, Türkiye Hatay, of Microbiology, of Medicine Department Faculty University Mersin 2

Mersin University Faculty of Pharmacy Department of Pharmaceutical Chemistry, Mersin, Türkiye Mersin, Chemistry, of Pharmaceutical of Pharmacy Department Faculty University Mersin

methods and antimicrobial effects of these - com herapy of herapy bacterial and fungal infections is limited because of the increasing number of multi-drug resistance pathogens, such as m 1 Staphylococcus Staphylococcus aureus

T In this study, ten new 1,2-disubstituted benzimidazole Benzimidazoles carrying different substituents have vari- Benzimidazoles carrying have substituents different imidazoles: imidazoles: A New Profile of Biological Activities. Der Fungal Fungal Pathogens: Concern for Resistance beyond - Can dida albicans and Aspergillus . fumigatus nosocomial methicillin-resistant Staphylococcus aureus (MRSA) infection including previous use of - antimicrobi Chemoth 49: 999–1050, 2002. J Antimicrob als. REFERENCES 42: 4419, 2004. Pathak Pathak D, Siddiqui N, Bhrigu B, Alam Ahsan W, MS. Benz - Pfaller M, Diekema D. Rare and Emerging Opportunistic Graffunder EM, Venezia RA. Risk factors associated with SYNTHESIS AND OF EVALUATION ANTIMICROBIAL ACTIVITIES OF SOME tant derivatives were synthesized by conventional and microwave microwave and conventional by synthesized were derivatives synthesis pounds were tested by Microdilution Broth Method. in vitro Microdilution Broth by tested pounds were ous biological activities, i.e. anticancer, antiviral, antifungal, antihelmintic, anti-inflammatory, antihistaminic and - anti bacterial [3]. Also, benzimidazoles still remain one of most the versatile classes of compounds against C-2 and - microorgan N-1 in substitutions that shown was it Recently, isms. positions of benzimidazole ring were important for - antimi activitiescrobial [4,5]. creased creased by the irrational use of antimicrobial drugs. Hence, there is a need for effective alternative antimicrobial - com of the methicillin treatment for pounds such as vancomycin, these infections. 3. 1. 2. POSTER PRESENTATIONS sulfuric acid. Another synthesis method of 1,3,4-oxadiazole of method synthesis Another acid. sulfuric and acid polyphosphoric triphenylphosphine, anhydride, triflic chloride, thionyl oxychloride, pentoxide,phosphorous phosphorous as such reagents different a with hydrazines - 1,2-diaroyl or 1,2-diacyl of cyclodehydration the includes concepts these of One derivatives. 1,3,4-oxadiazole - cycliza of tion the about reported are methods synthesis Many i, nlei, ninlmaoy n atcne activities. anticancer and antiinflammatory analgesic, antituberculo sis, antimicrobial, as such activities biological of spectrum broad exhibited derivatives 1,3,4-oxadiazole 3. 2. 1. H 3 I CO P.NJP. Best, DJ. PJ.Brown,Cassels, R. Broom, Bhanlon, TJ. F. Macaev, G. Rusu, S. Pogrebnoi, A. Gudima, E. Stingaci, L. S. Rollas, H.Erdeniz. N.Gulerman, Farmaco 57:171,2002. 1997. 2563, 40: Chem Med J Wilson.NF.JM. Osborne,Mitchell, Bioorg Chem13:4842,2005. Med Reynoldsd. R. Dimoglo, A. F.Kandemirli, Shvets, N. Vlad, REFERENCES 1 Marmara University, SYNTHESIS AND CYTOTOXIC ACTIVITY OF HYDRAZIDE HYDRAZONES HYDRAZONES HYDRAZIDE OF ACTIVITY CYTOTOXIC AND SYNTHESIS AND THEIR CORRESPONDING 3-ACETYL-2,5-DISUBSTITUTED-1,3,4- CORRESPONDING THEIR AND in n hraetcl hmsr. hrfr several Therefore chemistry. pharmaceutical in application their to due importance gained have rings the years, recent n Kadriye 2 Marmara University, A kdağ O N International Symposium onDrugResearch &Development 2011 H

Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 34668İstanbul, Türkiye ie ebrd 1,3,4-oxadiazole membered five 1 1 , Sevgi

Faculty ofPharmacy, DepartmentofPharmaceutical Biotechnology, K Suna ÖZBAŞ arakuş O N H Oxadiazolines N 34668İstanbul, Türkiye 1 ,

Bedia T DRD 2011 Ar uran P-032 1-2 86 Koçy -

7. 6. 5. 4. bromide] assay. [3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium MTT of line cell HEK293 using by evaluated been have pounds reagent like sulfuric acid, phosphorous oxychloride.phosphorousacid, sulfuric reagentlike aromatic acids or aromatic aldehydes by using a dehydrating is that the acid hydrazides are cyclization with acid chlorides, antiinflammatory. and anticanceranti-HIV, antiviral, antimicrobial, as such ties - activi pharmacological various exhibit be to known were Hydrazide-hydrazones anhydrides. acetic with (1) drazones azolines (2) were synthesized by cyclization of hydrazide-hy - 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadi research, 2 , Jülide 3 CO İ B. Koçyigit-Kaymakcıoglu, E. Oruc, S. Unsalan, F. Kande F. Unsalan, S. Oruc, E. Koçyigit-Kaymakcıoglu, B. SAF. Med Shalaby,MA. El-Demellawy.MA.J Rostom, Eur Pharm Arch El-Ashry. EH. El-Sayed, WA. Abdel-Aal, MT. Liras,S. MP. 437, SynthCommun30: Segelstein. BE. Allen, 1253, 2006. Shvets,N. mirli, Dimoglo.Rollas,A. S. 41: Chem Med EurJ Chem 38:959,2003. Chem Life 339:656,2006. Sci 2000. ğ İ t K aymakçıoğlu A kbuğa 5-7 yooiiy f h snhszd com- synthesized the of Cytotoxicity 2

O N H 1 , Sevim 2 R ollas O N 1 N , Ar O 3-4 H In this In C H 3 - - POSTER PRESENTATIONS -

3 values of studied compounds were determined a Yüksel ALTUN , Yüksel 8.180±0.135) was given in Figure 1. in Figure given 8.180±0.135) was a 1, 2 k/pH data pairs by means of the non-linear regression NLREG graphic of 1. sertindoleNLREG graphic Figure in 42.5% (v/v) ace tection. J Chromatogr B 856: 20-28, 2007. B 856: 20-28, tection. J Chromatogr 2007, (http://www.nlreg.com). Program, Curve Fitting The The pK Sherrod Sherrod PH, NLREG, Nonlinear Regression Analysis and tonitrile-water mixtures. 2. from from of sertin NLREG graphic NLREG an [2]. example, As - program dole (pK plc - - 87 H P-033 DRD 2011 DRD C. o Bediha YALÇIN , Bediha 1, * *[email protected] VALUES OF FOUR ANTIPSYCHOTIC DRUGS B a K Senem ŞANLI Senem International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International X-Terra RP-18 X-Terra column (250x4.60 mm values of four antipsychotic drugs, a Department of Chemistry, Faculty of Science and Arts, Hitit University, Çorum, Türkiye University, and Arts, Hitit of Science Faculty Department of Chemistry, 1

ntipsychotic ntipsychotic agents are used in psychiatric pa- episodes of psychotic the management for tients as well as for other behavioral symptoms such as

Gazi University, Gazi Faculty of Education, Department of Chemistry, 06500 Teknikokullar, Ankara, Türkiye Ankara, 06500 Teknikokullar, Department of Chemistry, of Education, Gazi Faculty Gazi University, 3 DETERMINATION OF p nation nation of five antipsychotic drugs in rat plasma by high performance liquid with chromatography ultraviolet de REFERENCES In this study, pK

Zhang G, Terry Jr AV, Bartlett MG. Jr Zhang Terry Simultaneous AV, G, - determi A Department of Analytical Chemistry, Faculty of Science and Arts, Ondokuz Mayıs University, Kurupelit, Samsun, Türkiye Samsun, Kurupelit, University, Mayıs Ondokuz Arts, and Science of Faculty Chemistry, Analytical of Department 2 and the column temperature was 25 was temperature used and the column m) was IDx5 namely; sertindole, olanzapine, clozapine and risperidone were determined in 42.5% (v/v) acetonitrile-water mixtures using LC-UV method. 1. agitation. agitation. Second generation antipsychotics (SGAs) (such as sertindole, olanzapine, ziprasidone and risperidone) are popular for the treatment of schizophrenia and other psy choses in the clinic [1]. POSTER PRESENTATIONS The IC The lear cells of acute lymphoblastic leukemia patients (ALL-MC). mononuc and (P3HR1) lines cell B-lymphoma HL60), (K562, lines cell leukemia chronic in method MTT colorimetric by evaluated were compounds these of effects cytotoxic The 1). (figure Pharmacy of Faculty University, Istanbul by sized synthe first are that derivatives thiosemicarbazone) tuted 3-(N-substi- 5-trifluoromethoxy-1H-indole-2,3-dione new of potential anticancer investigated we study, this In effects. antiproliferative high show derivatives containing groups trifluoromethoxy and methoxy 5-halide, lines, cell cancer human several against inhibitors growth as in developed analogs 5-substituted the among particular, In developed. were agents anticancer result, a as and compounds related of synthesis extensive to decade past the in led carbazones thiosemi - 1H-indole-2,3-dione active biologically numerous ie wr eautd y oprn IC comparing by evaluated were tives deriva- thiosemicarbazone of Effectiveness index. totoxicity cy to according curve dose-response from calculated were cell lines. Also, to investigate apoptotic mechanism of these of mechanism apoptoticinvestigate to Also,lines. cell 4 DepartmentofPediatric Hematology andOncology CYTOTOXIC AND APOPTOTIC EFFECTS OF NEW 5-TRIFLUOROMETHOXY- NEW OF EFFECTS APOPTOTIC AND CYTOTOXIC T 2 Department ofPharmaceutical Chemistry, Faculty ofPharmacy, İstanbul University, Beyazıt-İstanbul, Türkiye 1 50 H values (IC values 1 -INDOLE-2,3-DIONE THIOSEMICARBAZONES ON LYMPHOMA AND LYMPHOMAAND ON THIOSEMICARBAZONES -INDOLE-2,3-DIONE ily hi atcne atvt. h dsoey of discovery The activity. anticancer their cially espe activity biological potential high their for interests great drawn have hiosemicarbazones Department ofPhysiology, Istanbul Faculty ofMedicine,İstanbul University, Çapa-İstanbul, Türkiye Serap ERDEMKURUCA 3 DepartmentofBiology, Faculty ofScience, İstanbul University, Beyazıt-İstanbul, Turkey 50 is a concentration that kills 50% of cells) of 50% kills thatconcentration a is International Symposium onDrugResearch &Development 2011 50 1,* aus n leukemic in values LEUKEMIA CELL LINES CELL LEUKEMIA , NilgünKARALI *[email protected] Zeynep KARAKAŞ , İstanbul Faculty ofMedicine,İstanbul University, Çapa-İstanbul, DRD 2011 P-034 Türkiye 88 - - - - C 4-FC stituted thiosemicarbazones) potential andchronic inB-lymphoma leukemia. drug chemotherapeutic have might 3-thiosemicarbazones 5-trifluoromethoxy-1H-indole-2,3-dione- result, a As lines. cell cancer tested all in effective was thiosemicarbazone) 5-trifluoromethoxy-1H-indole-2,3-dione-3-(N-allyl that ing through caspase3 apoptotic pathway. It was interesting find- occurs be may mechanism effect thinkable, is It ALL-MC. in totoxicdifferentlittle in and cellline P3HR1 in ranges(<5ug) on P3HR1 cells.performed All of compounds were found cy was staining immunohistochemical caspase3 compounds, 2 , Kadriye AKGÜN DAR 6 H = CH R= 3-(N-sub 5-Trifluoromethoxy-1 H-indole-2,3-dione 1: Fig 5 4-CH , 6 H 4 , 4-NO 4 3 C , 3 C 2 6 2 H H C 5 6 4 CH , H 4-CH , 4

OCF N 2 H -CH=CH 3 3 O OC 3 , EbruGÜREL N 6 H 2 N 4 cyclo-C , 4-BrC , H R N S H 6 6 H H 4 11 4-ClC , 3 , C , 6 H 5 CH 6 H 2 4 - - , , POSTER PRESENTATIONS - - ils O ssential E of

In In this quorum study, sensing inhibitor (QSI) of potential SPS. Plant-based anticancer molecules: A chemical and biological profile of some important leads. Bioorganic & Medicinal Chemistry 2005. 13:5892-5908, L, Calum H, Hentzer M, Hougen Rygaard HP, J, Moser C, Eberl L, Hoiby N and Givskov M. Garlic blocks quorum clearingpulmonary- of rapid Pseu promotes and sensing 3873- 151: Microbiology infections. aeruginosa domonas 3880, 2005. QS by vanilla extract. in Letters Applied Microbiology 42: 637-641, 2006. Srivastava V, Singh NA, Kumar JK, Gupta MM and Khanuja and MM Gupta JK, Kumar NA, Singh V, Srivastava Bjarnsholt T, Jensen PO, Rasmussen TB, Christophersen Choo JH, Rukayadi Y, Hwang JK. Inhibition of bacterial lating lating QS using this communication system in pathogenic bacteria. QS inhitor activities of natural oils were screened using four kinds of biomonitor organisms; Quorum Sensing Inhibitor and Chromobacterium vio Selector (QSIS1) strain1 laceum strain CV026, C. violaceum VIR07 strain and C. violaceum strain 12472. ATCC Rose, clove, pinus and chamomile essential oils were showed significant inhibitor activities for very at concentrations. low tested strains all biomonitor twenty essential oils was investigated to find natural and non- and natural find to investigated was oils essential twenty in modu may reveal ompounds candidate QS toxic inhibitor 4. 5. 6. Rümeysa ERİŞ , Rümeysa * Activities 89 P-035 DRD 2011 DRD *[email protected] nhibitor I Seyhan ULUSOY Seyhan ensing International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International S Türkiye Isparta, 32260 University, Demirel Süleyman of Biology, Department

uorum Q acterial cell to cell communication sensing (QS), or N-acyl-L-homoserine lactone quorum based signalling system, coordinates a wide variety of

cal Microbiology 12: 564-582, 1999. Reviews mara mara M, Daykin M, Stewart Lamb SwiftJ.H, S, Bycroft BW, GS, Williams P. Quorum sensing and Chromobacterium violaceum: Exploitation of violacein production and inhibition for the detection of N-acylhomoserine lactones. Microbiology 143: 3703-3711, 1997. mond GP. Quorum-sensing in Gram-negative bacteria. 2001. FEMS Microbiology 25: 365-404, Reviews REFERENCES Cowan MM. Plant Products as Antimicrobial Agents. Clini- Agents. Antimicrobial as Products Plant MM. Cowan - SR, A, Ca Chhabra Taylor L, MK,Winson Fish McClean KH, Whitehead Whitehead NA, Barnard AM, Slater H, Simpson NJ, Sal- B functions in Gram-negative bacteria, including antibiotic and exoenzyme production, biofilm formation, violacein production1-2. Thus, manipulating this communication - sys tem could provide an opportunity to modulate bacterial QS dependent traits such propertiesVarious as pathogenity. of plant based products most studied; antibacterial3, - antican 4, and anti-QScer properties. 5-6 3. 2. 1. POSTER PRESENTATIONS culture andfood technology. agri- medicine, as such fields, different many in application find and bacteria antibiotic-resistant multi with combat in hope new offer may systems QS bacterial of Inhibition [3,4]. therapy antimicrobial for target attractive an system QS the makes production factor virulence and pathogenicity their regulate to QS employ bacteria pathogenic many that ery density.discov population The cell own its monitor to rium on the production of signal molecules which enable a bacte depends QS determinants[1,2]. virulence of production the and conjugation swarming, synthesis, antibiotic formation, biofilm including species, bacterial Gram-negative and itive 3. 2. 1. D Hentzer M, Wu H, Andersen JB, Riedel K, Rasmussen TB, Rasmussen K, Riedel JB, Andersen H, Wu M, Hentzer - Sal NJ, Simpson H, Slater AM, Barnard NA, Whitehead Pesci EC, Pearson JP, Seed PC and Iglewski BH. Regulation Bagge N, Kumar N, Schembri MA, Song Z, Kristoffersen P,Kristoffersen Z, Song MA, Schembri N, Kumar N, Bagge ReviewsFEMS Microbiology 25:365-404,2001. bacteria. Gram-negative in Quorum-sensing GP. mond 179:3127-3132,1997. ofBacteriology nosa. Journal aerugi- Pseudomonas in sensing quorum rhl and las of REFERENCES P 2 an array of phenotypes in a variety of Gram-pos - of variety a in phenotypes of array an or quorum sensing (QS) has been shown to regulate communication cell-cell dependent ensity Department of rofens 1 DepartmentofBiology, Süleyman Demirel University, 32260Isparta, Türkiye International Symposium onDrugResearch &Development 2011 I

nterferes Clinical Microbiology, Faculty ofMedicine,Marmara University, İstanbul, Türkiye Seyhan ULUSOY P seudomonas

with *[email protected] 1,* , GülgünBOŞGELMEZTINAZ DRD 2011 P-036 C 90 - - ell infections incombination withconventional antimicrobials. could be a choice to the treatment of pseudomonal bacterial and vitro in activity inhibitory swarming and elastase have andswarmingmotility.production elastase on inhibition significant to showed NSAIDs strain. of production pyociyanin and elastase fects of these drugs on swarming motility, biofilm formation, ed hydratefenoprofensalt wereinvestigatsodium, calcium en naprox ketoprofen, indomethacin, ibuprofen, flurbiprofen, as such (NSAIDs) drugs flammatory 4.

aeruginosa Wu H, Song Z, Hentzer M, Andersen JB, Molin S, Givskov S, Molin JB, Andersen M, Hentzer Z, Song H, Wu using biomonitor strains. A strains. biomonitor using u fnig sget ht ilfnc n ketoprofen and diclofenac that suggest findings Our of potentials anti-QS study, this In crobial Chemotherapy 53:1054-1061,2004. Antimi- of Journal mice. in infection lung aeruginosa nas Pseudomo in clearance bacterial quorum- enhance and inhibit sensing furanones Synthetic N. Hoiby and M tors. The 22:3803-3815,2003. EMBOJournal inhibi- sensing quorum by virulence aeruginosa monas PseudoAttenuationGivskovof M. N, Hoiby S, Kjelleberg P,Steinberg L, Eber S, Molin JW, Costerton M, Manefield -C ell C ommunication 1,2 nd further examined the ef- the examined further diclofenac sodium salt, sodium diclofenac nonsterodial anti-in - nonsterodial PAO1 aeruginosa P.

- - - - POSTER PRESENTATIONS ------search search Group: The effect of intensive treatment of diabetes on the of and development long-term progression complications in insulin-dependent diabetes mellitus. N Engl J Med 329:977–986, 1993. ery systems. Curr Opin Investig Drugs. 11(4):394-401, 2010. 11(4):394-401, Drugs. Investig Opin Curr systems. ery Strack T. The pharmacokinetics of alternative insulin deliv insulin alternative of pharmacokinetics The T. Strack 3. 19 patients were prescribed with only one insulin brand, only 5 only brand, insulin one only with prescribed were patients 19 were patients Other a day. once insulin injecting were patients respec n=1, n=1, (n=19, day a injections 4 or 3 2, administering with were unsatisfied were of the percent four patients Fifty patients tively). the of 42.3% and injection as insulin administering injec Insulin public. in insulin injecting while discomfort pop feeling most however patients, the of 73% by easy as stated is tion was transdermal of administration route insulin ular preferred (46.2%), injection Painful (30.7%). route and oral (42.3%) patch insulin with problems (38.5%) patients carrying/handling and of fre administration complains major the were (26.9%) quency de 90 with insulin injecting patients the of majority A injection. and (65.4%) injecting while skin squeezing (73.1%), angle grees Patients (57.7%). swap alcohol with site cube, ice administration on, cleaning (carrying storage insulin about on dose knowledgeable were insulin tapering were patients the of 26.9% refrigerator). Majority monitoring. sugar blood home to according own their of injection insulin about 53.8% knowledge their gather of the addition, patients In (26.9%). nurses and (53.8%) about physicians from (primarily insulin about informed were (n=14) [57.1%]) patients the dosing and [57.1%] technique injection (n=10) [71.4%], patients the storage of 38.5% visits. further in pharmacists their by treat drug about (primarily diabetes about informed also were of [50%], ment complications diabetes [70%], hyperglycemia Convenience by [40%]) pharmacists. their and [40%] foot-care more were the take that patients and of ease use are the concerns main should Pharmacists administration. insulin for looking injection for insulin especially role in active education patient care. diabetes in technique ------91 P-037 . . The DRD 2011 DRD 3 . However, . However, . . An inten 1 2 * [email protected] Özlem ÇOBAN, Özlem Emine TAŞHAN, , Hasan KACAMER, * Türkiye Ankara, of Pharmacy, Faculty University, Hacettepe Aygin BAYRAKTAR Aygin KARATAŞ, Nuray LÜLECİ, Zeynep International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Kutay DEMİRKAN Kutay

he he accuracy and convenience of pen devices for of quality patient’s improved have injection insulin life in mellitus diabetes (DM) treatment DIABETIC WITH SATISFACTION INSULIN PATIENTS’ INJECTION T REFERENCES lin-pen treatment, quality of life and metabolic control: Retrospective intra-group evaluations. Diabetes Res Clin 10:221–230, 1990. Pract. A total of 26 patients (77% female) with average age of 54 average with female) (77% of A 26 patients total Diabetes Diabetes Control and Complications Trial (DCCT) Re Hornquist JO, Wikby A, Andersson PO, Dufva AM. Insu- 2. 1. years old (range 9-71) completed the questionnaire. Seventy-sev questionnaire. the completed 9-71) (range old years sive sive insulin therapy for a better glycemic control in diabetic patients requires multiple daily insulin injections mic including oral, control, inhaled, buccal, nasal, and patch new for attempts years, recent in advances the Despite routes. formulations have been faced with certain limitations technique administration its and injection insulin on isfaction for assessed were patients The DM. with patients the amongst han and use administration, of route the on preferences their dling of insulin and injections about for sources information question the 15-items by using therapy and insulin diabetes were naire. Questionnaires to distributed the patients when they visited the were Four pharmacies se retail pharmacies. lected according to location of externship of the pharmacy by filled and read were questionnaires The Ankara. in students during 2011) (March month one in students pharmacy senior period. externship pharmacy community their average the and diabetes II type had patients the of percent en Despite years). 1-30 (range years 11.1 was of diabetes duration patient compliance patient has compliance really been a major concern for this of routes alternative Several insulin. of administration of route glyce effective an for consideration under are administration and sat aim preferences of this study was to patient’s assess POSTER PRESENTATIONS e eetrpoei (CE ad irnces M) assays (MN) micronucleus and (SCGE) electhrophoresis gel (n=4). cell single The cultures(WBCs) blood whole human in evaluated been have mg/L) 400 to (0 QTP and RPD OLZ, of ture system. Therefore, in this study, the genotoxic potentials cul- lymphocyte human on QTP and RPD OLZ, of potentials edge, there is scarce data considering the genotoxic damage - knowl best our Tosystems. cardiovascular and nervous on indicatedreports that these drugs could exhibit toxic effects recent However, (BD). disorders bipolar and schizophrenia 1 T Kahramanmaraş Sütçü İmam University, Medical Faculty, Department of Microbiology, 46100 Kahramanmaraş, Türkiye Hasan he O

genotox 5 Atatürk University, Medical Faculty, Medical Pharmacology Department,25240Erzurum,Türkiye TÜ n ae omny sd o te ramns of treatments the for used commonly are and drugs antipsychotic atypical are que (QTP) tiapine and (RPD) risperidone (OLZ), lanzapine 3 Atatürk University, Medical Faculty, Medical GeneticsDepartment,25240Erzurum, Türkiye rkez 6 Atatürk University, Medical Faculty, Biochemistry Department,25240Erzurum,Türkiye 4 2 Atatürk University, Medical Faculty, Psychiatry Department,25240Erzurum,Türkiye Atatürk University, Faculty ofScience, Biology Department,25240Erzurum,Türkiye Ahmet 2 , Başak I c International Symposium onDrugResearch &Development 2011

potent H acım T ogar Ü on ft I 2 , Abdulgani als

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T 92 lymphocytes - atar sured. thatfects are toexpolikely doses the on depending appear ef- cyototoxic the consider to necessary is safely,it used but be can drugs antipsychotic atypical different three tested the that concluded is It cultures. lymphocyte of sterility to caused above) and mg/L (250 concentrations drug highest the of application However,the (P>0.05). values control the and MN/1000 cell were not found significantly different from assay) SCGE (for damage DNA showing cells of scores total the of values mean the fact, In genotoxicity. induce not did drug antipsychotic tested the that indicated study present were applied to estimate the DNA damage. The results of the G

3 atyp , Ebubekir ey İ ko I Ğ c lu

anth 2 DİRİCAN , M.Sait I psychot K 1 , ele

İsmet Ş 6 K ırkpınar I c

drugs 4 ,

- POSTER PRESENTATIONS - were were

2 c Türkiye Türkiye I enotox (L.) G

lichen extracts in mercury- As conclusion, conclusion, As intestiniforme. D. forme I 11 nduced induced genetic damage on human lym- n I 2 I de I D. D. intestiniforme provided increased resistance of DİRİCAN ntest I hlor C phocytes. alleviated by the presence of of presence the by alleviated the results of present study revealed for the first time that the lichen DNA against HgCl Dermatocarpon Dermatocarpon intestiniforme ex chromatid sister The (n=3). cultures blood human treated performed were assays (MN) micronucleus and (SCE) change to assess DNA damages in lymphocytes. Our results clearly revealed that, the SCE and MN rates induced by HgCl - - 93 Ebubekir , Ebubekir 2 P-039 DRD 2011 DRD rkez ercury TÜ M ermatocarpon nst Hasan I D : ) and the role of aqueous 2 Aga International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Damage

Department of Biology, Faculty of Sciences, Atatürk University, 25240 Erzurum, Türkiye 25240 Erzurum, Türkiye University, Atatürk of Sciences, Faculty Department of Biology, 2 ercury has been used in many domains of human activities for many years, although in any form of mercury is reported to be On toxic. the odulator

A M M Kahramanmaraş Sütçü İmam University, Medical Faculty, Department of Microbiology, 46100 Kahramanmaraş, Kahramanmaraş, 46100 Microbiology, of Department Faculty, Medical University, İmam Sütçü Kahramanmaraş 1 other hand, lichens have been used in the treatment of sev eral eral diseases such as tuberculosis, hemorrhoids, ulcer, - dys entery and Animal cancer. investigations on some common - anti and antioxidant their demonstrated have species lichen the on data veryscarce is there However, activity. mutagenic medical or biologic effects of specific lichen species. There fore, in the present study, we assessed the cyotogenetic effects of mercuric chloride (HgCl POSTER PRESENTATIONS the micronucleus (MN) assay was carried out. Nuclear divisi- Nuclear out. carried was assay (MN) micronucleus the extracts alga aqueous of effects aneugenic or clastogenic determine to order in Therefore, cells. blood human tured of effects biochemical and genotoxic the assess to performed was study no knowledge, best our of rivers and lakes some in available abundantly algae green hand, other the On ders. ases cancersincluding certain and neurodegenerative disor dise serious cause to thought been have metabolites these don’texactly.Moreover, explain properties and pharmacological toxic this But, properties. pharmacological also have S 3 Atatürk University, KazımKarabekir Education Faculty, DepartmentofBiology, 25240Erzurum,Türkiye Hasan T organisms, animals and humans but some of them of some but humans and organisms,animals aquatic to threat a pose that metabolites toxic of variety a produce to known are species alga everal he , generally found in found generally , P 2 otentials E Department ofBiology, Faculty ofSciences, Atatürk University, 25240Erzurum,Türkiye 1 Kahramanmaraş Sütçü İmam University, Medical Faculty, Department of Microbiology, T valuation ürkez International Symposium onDrugResearch &Development 2011 is a genus of filamentous of genus a is Ulothrix 2 , Hasan water and water fresh

on cul- on tenuissima U. of G

U ürbüz

lothr the 46100 Kahramanmaraş, Türkiye marine . ToTurkey. G 3 , Elanur enotoxic I DRD 2011 and P-040 x

94 tenu - - sterility at higherconcentrationssterility dueto oxidative stress. to caused but non-genotoxic be to found was tenuissima U. in observed TACand conclusion,rates. TOSNDI In and levels were alterations dose-dependent But endpoint. notoxicity any statistically important changes in the rates of studied ge ppm) for 72h. Our results showed that this alga did not cause were added to cultures at different concentrations (0 to 5000 species this of extracts aqueous The 2010. year the of riod pe summer in Turkey) (Erzurum, Hasankale in Pond Porsuk three healthy persons. The alga samples were collected from from samples blood heparinized obtained we aim this For effects. oxidative determine to examined were [TOS]) stress oxidative total and [TAC] capacity antioxidant (total meters para - biochemical addition, In evaluations. cytotoxicity for analyzed also was lymphocytes peripheral in (NDI) index on A ydın I ss 2

, Ali and I ma A slan Oxidative (KU 3 tz , Ebubekir .) I n VI Damage DİRİ tro can 1

- - POSTER PRESENTATIONS - - in (G-6-PDH) intestiniforme aug- D. IN VITRO 2 lichen diet may play a protective role in the ürkez T matid matid exchange (SCE) rates and main antioxidant enzyme activities including superoxide dismutase (SOD), catalase (CAT) and glucose-6-phosphate dehydrogenase negative any exhibite not did concentrations tested tracts at effects on above studied parameters in culture tubes with or without adding S9 the mix. results Moreover, of the - pres and frequencies SCE of increases the that indicated study ent were enzymeAFB1 activitiesby antioxidant of decreases the and 25 (at extracts lichen the of application the by minimized 50 µM). Our results firstly suggest that ments the antioxidants defense against AFB1 induced tox icity. Again, these results demonstrate that dose controlled D.intestiniforme of AFB1 mutagenesis and/or carcinogenesis. process AFB1 (10 µM) and lichen (1, 5, 10, 25, 50 and 100 µM) treated treated µM) 100 and 50 25, 10, 5, (1, lichen and µM) (10 AFB1 human whole blood cultures (n=3) for 72h. The lichen ex , Hasan (A LICHEN) MODULATES AFLATOXIN 1 - - - 95 P-041 DRD 2011 DRD DİRİCAN extracts conferred a Ebubekir Ebubekir Aspergillus , parasiticus exhib and International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

D. D. intestiniforme

Atatürk University, Faculty of Science, Department of Biology, 25240 Erzurum, Türkiye 25240 Erzurum, Türkiye of Biology, Department of Science, Faculty University, Atatürk 2

B1 INDUCED GENETIC AND OXIDATIVE DAMAGE ecent ecent reports suggest that aflatoxin B1 (AFB1), a by produced foods of contaminant toxic worldwide Aspergillus flavus in the presence or absence of mixed function mixed of absence or presence the in vitro in R Kahramanmaraş Sütçü İmam University, Medical Faculty, Department of Microbiology, 46100 Kahramanmaraş, Türkiye Kahramanmaraş, 46100 Microbiology, of Department Faculty, Medical University, İmam Sütçü Kahramanmaraş DERMATOCARPON INTESTINIFORME 1 its an oxidative stress mediated genotoxicity although, the been not has AFB1 by caused damage cellular of mechanism ascor as such molecules antioxidant Several elucidated. fully bic acid, beta-carotene and tocopherol have been shown to possess anti-carcinogenic and anti-mutagenic properties against AFB1 toxicity. On the other hand, lichens have long been investigated popularly for biological roles; mainly antimicrobial and antioxidant activities. Also, the influence of lichenic substances on DNA binding of AFB1, in mammalian cells, is still unknown. Therefore, in this study, we aimed to determine whether protection against AFB1-induced genotoxic and oxidative damage oxidases (S9 mix). For this aim, we determined sister chro POSTER PRESENTATIONS against LN toxicity using micronucleus (MN) test and nuclear to investigateundertaken the in vitro protective effect of AA was study present the Therefore,vitro. in toxicity LN on AA of role the examine to performed was study no knowledge, tions and is a powerful water-soluble antioxidant. To our best ac nonenzymatic several has (AA) acid ascorbic view, other In models. test simplistic of basis the on assumed quently fre is products care health oral of profile safety biologic the 1 Kahramanmaraş Sütçü İmam University, Medical Faculty, Department of Microbiology, 46100 Kahramanmaraş, Türkiye L THE EFFECTS OF ASCORBIC ACID ON LISTERINE TOXICITY IN VITRO IN TOXICITY LISTERINE ON ACID ASCORBIC OF EFFECTS THE scarce data is available in the literature. Moreover,literature. the in available is data scarce although properties anti-bacterial and anti-fungal has rinse, mouth used commonly a (LN), isterine 4 2 Atatürk University, Faculty ofDentistry, DepartmentofPeriodontology, 25240Erzurum,Türkiye Atatürk University, Medical Faculty, DepartmentofMedical Genetics,25240 Erzurum, Türkiye Abdulgani 3 Atatürk University, Faculty ofScience, DepartmentofBiology, 25240Erzurum,Türkiye International Symposium onDrugResearch &Development 2011 T atar 2 , Hasan T ürkez DRD 2011 P-042 96 3 - - , Taner ent study. pres- the in time first the for indicated was toxicity induced LN- minimizing in AA of role ameliorating the conclusion, In alone. LN with treated group the to compared as rates NDI However,resultedLN co-treatmentand AA increasesof in of NDI. significantdecreasesof statistically caused but mations for MN induce not did LN that, showed study present the of results The72h. for cultures blood human whole to plied wereµM) ap 10 and (5 AA and ml/culturev/v) of 100% to (0 LN of concentrations Different analysis (NDI) index division A rabacı 4 , Ebubekir DİRİCAN 1 - - POSTER PRESENTATIONS . The The . -1 g mL mg , respectively. -1 mg mL 1,* All necessary validation parameters and system suitability system and parameters validation necessary All , Sibel A. ÖZKAN LOD LOD and LOQ values are 0.004, 0.013 was chosen as the internal standard (IS). The proposed HPLC HPLC proposed The (IS). chosen was as standard the internal a 11.48 good between method resolution GEM gives and in- - con these Using time. analysis short a within standard ternal obtained as times 3.20 IS, were min for the retention ditions, GEM. 4.25 min for test results were obtained as details. Linearity was obtained 20 and 0.25 between range concentration the in Also Also interday and intraday studies realized and 0.069 % and 0.101 % RSD values, respectively, show the precision of this Also method. this method validated applied - pharmaceu for tical and formulations the of results recovery tests found are is method the that shows recovery percentage High %. 99.96 excipients used commonly the of interferences the from free and additives in the formulations of drugs. The proposed method is suitable for quality control laboratories, where essential. and time are economy 1,2 - - - - 97 P-043 DRD 2011 DRD C. Granisetron Granisetron C. o [email protected] * Mehmet GÜMÜŞTAŞ with a mobile phase of methanol– International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International OF GEMIFLOXACIN FROM TABLET DOSAGE FORM

Hitit University, Science and Literature Faculty, Department of Chemistry, 19040 Çorum, Türkiye 19040 Çorum, Department of Chemistry, Faculty, and Literature Science Hitit University, emifloxacin emifloxacin (GEM) 4-methoxyimino-pyrrolidin-1-yl]- 1-cyclopropyl- 7-[(4Z)-3-(aminomethyl)- 6-fluoro-4-oxo- 1,8-naphthyridine-3-carboxylic 2 Ankara University, Faculty of Pharmacy, Department of Analytical Chemistry, 06100 Ankara, Türkiye 06100 Ankara, Chemistry, Analytical Department of of Pharmacy, Faculty University, Ankara 1

The The aim of study this which work a pur presenting HPLC G DEVELOPMENT OFRP-HPLC VALIDATED METHOD FOR THE ESTIMATION tion. The compound has broad spectrum of activity against bacteria. and gram-negative gram-positive meth- accurate and precise sufficiently simple, rapid, a poses od for the determination of GEM, in raw material and phar maceutical formulations. For this reason method HPLC-DAD (X-Select RP- In reversed-phase a method; this developed. is 18 (250 x 4.6 mm ID x 5m) 25 at performed was separation matographic acid is a new fluroquinolone antibacterial compound with enhanced affinity for bacterial topoisomerase IV and it used for the of treatment respiratory and urinary tract is infec water (50:50 ;v/v), containing 15 mM phosphoric acid (pH 2.50 ) at 1.0 ml/min flow rate was used to separate GEM and internal standard (IS) with a detection of 272 nm. The chro POSTER PRESENTATIONS ain a promd t 25 at performed was ration respectively.IS, chromatographicsepa- and The GRA for nm 215 of detection a with compounds both separate to used was rate flow ml/min 1.0 hydroxide. sodium of addition by phoric acid. The pH of the mobile phase was adjusted at 2.50 phos- mM 15 containing ;v/v), (45:55 methanol–water were RP-18 (250 x 4.6 mm ID x 5m) (X-Select column reversed-phase a method; this In GRA. of receptors.rinic musca- or receptors dopamine on effect any have not does drug This sickness. motion to due vomiting on effect much have not does It oblongata. medulla the in center vomiting the activates that nerve a is which nerve, vagus the of tivity ac the reduce to is effect main chemotherapy.Its following vomitingtreattoand antiemetic nausea an as used tagonist was chosen as the internal standard (IS) because it showed it because (IS) standard internal the as chosen was G An HPLC-DAD method is presented for the determination DETERMINATION OF GRANISETRON BY HPLC-DAD TECHNIQUE IN IN TECHNIQUE HPLC-DAD BY GRANISETRON OF DETERMINATION 1 Ankara University, Faculty ofPharmacy, DepartmentofAnalytical Chemistry, 06100Ankara, Türkiye 2 HititUniversity, Science andLiterature Faculty, DepartmentofChemistry, 19040Çorum,Türkiye abxmd i a eooi 5H3 eetr an- receptor 5-HT3 serotonin a is carboxamide yl-9-azabicyclo[3.3.1]nonan-3-yl)-1H-indazole-3- 1-methyl-N-((1R,3r,5S)-9-meth- (GRA), ranisetron International Symposium onDrugResearch &Development 2011 with the mobile phase assayed o C. Hydrochlorothiazide (HCT) (HCT) Hydrochlorothiazide C. PHARMACEUTICAL DOSAGE FORMS DOSAGE PHARMACEUTICAL Mehmet GÜMÜŞTAŞ *[email protected] DRD 2011 P-044 98 - 1,2 control laboratories, where economy andtimeare essential. cal formulations. The proposed method is suitable for quality pharmaceuti - and material raw in GRA of determination the for method accurate and precise sufficiently simple, rapid, a purposes HPLCstudy present drugs.The of formulations the terferences of the commonly used excipients and additives in in- the fromfree is method the showsthatrecoverycentage per High BARND2. for % 100.19 and BRAND1 for % 100.16 found and products pharmaceutical different two applied are tests recovery of results Thecarried. were tests recovery HPLCproposed method,the of applicability and validity the centration0.25-15 rangeof con- the in obtained was Linearity 1.080. factor tailing 1,77; (α) selectivity 28572; number plate theoretical 10.03; is GRA of Resolution out. carried also were tests suitability System 3.30 minfor HCT, 4.19minfor GRA. Using these conditions, the retention times were obtained as standards. internal potential other to compared resolution, better and shapes peak better with time retention shorter a *, SibelA.ÖZKAN h pooe mto hs en xesvl validated. extensively been has method proposed The 1 g mL mg -1 . In order to demonstrateIn . - POSTER PRESENTATIONS ------

, was investigated for iosensors hemically B C 3 rug dental dental surgery sing D U of

Mehmet Ali ONUR , Mehmet idocaine tions. Anal. Lett 28(15): 2663-2671, 1995. Lett Anal. tions. local anesthetics including ester-type anesthetics in human plasma and urine by gas spectrometry with solid-phase extraction. chromatography-mass J Chromatogr B Biomed Sci 726 (1-2):185-94, 1999. Appl J, Watson AO, Uboh CE, Soma LR. Quantification of penicillin-G and procaine in equine urine and plasma using J high-performance Chromatogr liquid chromatography. B Biomed Sci 714(2): 269-76, 1998. Appl ric detection of procaine hydrochloride using carboxy In this work, potential application of electrochemical ac Ohshima T, Takayasu T. Simultaneous determination of Luo Y, McNamara B, Fennell MA, Teleis DC, May L, Rudy fluorimet and behaviour Retention MMF. Choi S, Shuang 2 L 5. 6. 7. sponse of the drugs were examined by a biosensor based on based biosensor a by examined were drugs the of sponse direct electrochemistry of hemoglobin (Hb) immobilized on self-assembled monolayer (SAM) modified gold electrodes electrode). (Au/MPA/Hb Hb showed enzymatic behavior on research, this In electrode. the surfaceof the to binding drug Amperometric and voltammetric studies showed that the exhibited good electrocat modified electrode (Au/MPA/Hb) high showed and lidocaine of reduction the for activity alytic sensitivity construction which leads to biosensor. of a drug the construction of drug The biosensors. electrocatalytic re sophisticated sophisticated and costly instruments and special 10. training sensitivityenjoying high with method the reasons, these For rapid, simple and accurate simultaneously is expected to be enzymeAmperometric established. - consid biosensors have erable potential for continuous monitoring of drugs or me fluids11. in biological tabolites the lidocaine, the to electrode modified chemically a of tivity most commonly used local anesthetic for a wide range of procedures particularly ------of 99

P-045 onstruction DRD 2011 DRD C or Gülçin BOLAT , Gülçin [email protected] * 1,* F esponse R Gamze TAN Gamze International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International lectrodes This This is because the quantitative de E Hacettepe University, Institut of Science, Dept. of Biology, 06800 Ankara, Türkiye Türkiye 06800 Ankara, Dept. of Biology, of Science, Institut University, Hacettepe Hacettepe University, Faculty of Science, Dept. of Biology, 06800 Ankara, Türkiye 06800 Ankara, Dept. of Biology, of Science, Faculty University, Hacettepe 1 3 Hacettepe University, Faculty of Science, Dept. of Chemistry, 06800 Ankara, Türkiye 06800 Ankara, Dept. of Chemistry, of Science, Faculty University, Hacettepe 2

ocal anesthetics are drugs that nerve conduction, when block they are applied locally to reversibly Howev 1. concentrations appropriate at tissue nerve

lectrocatalytic odified E M Ruzafa A, Pastor MC, Aguilar JL, Galimany R. nation Determi- of Plasma Levels of Bupivacaine by High-Perfor of certain local anaesthetics in pharmaceutical - prepara tency of Ropivacaine and Lidocaine. Research Journal of 4(1):1-4, 2010. Pharmacology Anesthe Whole Blood caine by in Gas Chromatography. siology 29(1): 110-12, 1968. mance Liquid Chromatography. Journal of Liquid Chro 14(15): 2937 – 49, 1991. matography Comparative Comparative in vitro Study of Relative Anesthetic Po REFERENCES Keenaghan JB. The Determination of Lidocaine and Prilo and Lidocaine of Determination The JB. Keenaghan Salch GA, Askal HF, Spectrophotometric determination

Tsirlis Tsirlis A, Karanikola DabarakisT, N, Liverdos K, Charisi M. L 2. 3. 4. 1. er the toxicity from an high excessively of concentration the stand- obstacle main as seems blood the in anesthetics local anesthet of degree Toxicity uses. medical their of front in ing ics are modulated by several factors including distribution/ plasma concentrations, overdosing, systemic absorption, relative vascularity of the injection site even the speed of the injection.may there In the toxicity the case of increasing occur many side effects particularly and cardiovascular neurological complications. termination of local anesthetics in blood and other - biologi cal materials are obviously around the considerable point in metabolism and distribution of these assessment of toxicity, drugs following various routes of 2,3. administration Various have drugs anesthetic local of determination the for methods chro liquid or gas spectrophotometry4, like developed been 8, chemiluminescence detectionfluorimetric7, 5,6, matography flow-injection 9. analysis Many of these methods mentioned above, require several time-consuming manipulation steps, POSTER PRESENTATIONS 9. 8. Mo Mo ZH, Lou J, Long XH, Xia ZL. Determination of procaine ben- procaine, of P.Determination Miroslav H, Paseková senius’ JAnal Chem358(4):556-558,1997. Freanalysis. flow-injection ion-pairing hydrochlorideby tion. Talanta 52(1):67-75,2000. detec chemiluminescence permanganate-induced with analysis injection sequential by tetracaine and zocaine 2001. 321-9, 919(2): A Chromatogr J. chromatography. reversed-phase liquid in additive an as methyl-cyclodextrin International Symposium onDrugResearch &Development 2011 DRD 2011 100 - - 11. 10. Harwood GWJ, Pouton CW. Amperometric enzyme bio enzyme Amperometric CW. Pouton GWJ, Harwood ad- pulse Differential ZZ. Leng GD, Jin XY, Hu CY,Wang vanced Drug Delivery Reviews 18(2):163-91,1996. vanced DrugDelivery Ad- metabolites. and drugs of analysis the for sensors Biomed Anal 30(1):131-39,2002. trode in pharmaceutical preparations and urine. J Pharm elec paste carbon procainemodified pumice a at of hydrochloride determination for voltammetry sorption - - POSTER PRESENTATIONS - - -

2 on

aylor T based

Palmer , Palmer 2 ć adi R scavenger

acetylcholinesterase Zoran , Zoran

2 alle D134H is a naturally occurring single nucleotide polymor nucleotide single occurring naturally a is D134H V phism (SNP) in humans. Paraoxon and Cyclosarin (analogue) and Cyclosarin phism (SNP) in Paraoxon humans. inhibition of D134H by was 2PAM 3-8 times slower than wt times 7 enzymewas inhibited Paraoxon of reactivation while 1. faster At the same time catalytic parameters for acetylthio choline hydrolysis were not affected by the mutation sug- could reactivation and inhibition in acceleration that gesting be related to different transition state geometries in those out residues that points study this of Results reactions. three side the active center influence inhibition, reactivation and rates. catalysis human

- 101 , Anne 2 P-046 DRD 2011 DRD 2010. variant organophospate *[email protected]

ochran C Diego, La Jolla, CA 92093-0636, USA Diego, La Jolla, CA occurring 187: 238-240, 187:

, Rory 1,* catalytic

International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International naturally

a Hacettepe University, Faculty of Pharmacy, Dept. of Biochemistry 06100 Ankara, Türkiye 06100 Ankara, Dept. of Biochemistry of Pharmacy, Faculty University, 1Hacettepe üçükkilinç K

rganophosphates rganophosphates (OPs) are chemicals very that are poisonous widely used acetyl - inhibit OPs in agents. nerve in found are agriculture and

Tuba Tuba onstructing D134H, G, Radić Z, Taylor P. Investigating the structural influence G, P. Radić Taylor Z, of surface mutations on acetylcholinesterase inhibition by organophosphorus compounds and oxime - reactiva Interactions Chemico-Biologico tion. REFERENCES Kucukkilinc T, Cochran R, Kalisiak J, Garcia E, Valle A, Amitai Amitai A, Valle E, Garcia J, Kalisiak R, Cochran T, Kucukkilinc

Dept. of Pharmacology, Skaggs School of Pharmacy & Pharmaceutical Sciences,University of California at San of California Sciences,University of Pharmacy & Pharmaceutical Skaggs School 2Dept. of Pharmacology, O C tein sequence in order to convert human AChE into catalytic catalytic into AChE human convert to order in sequence tein one per molecules OP multiple inactivate will that scavenger molecule of scavenger. cholinesterase cholinesterase (AChE) and butyrylcholinesterase (BChE) by forming covalent chemical bonds through a process called phosphorylation. Use of human cholinesterase-oxime - cou ples of varying structure serving as catalytic bioscavengers poisoning. OP of treatment in approach therapeutic new a is pro AChE in mutations specific site generate to was goal Our 1. POSTER PRESENTATIONS ad wr etatd rm lsa y iudlqi extrac liquid–liquid by plasma from extracted were dard) secretion from thepancreas1,2. insulin stimulating by levels glucose blood lowers that tive deriva- amino-acid an is It mellitus. diabetes II type of ment the determination ofnateglinide inhumanplasma. 1. Ezgi UĞURLU A Physicians’ Desk Reference (PDR). 63 (PDR). Physicians’Reference Desk aelnd ad aelnd-hnl 5 itra stan- (internal d5 nateglinide-phenyl and Nateglinide Nateglinide is a novel oral glucose regulator for the treat NJ, 2009,p. 2314-2316. REFERENCES DETERMINATION OF NATEGLINIDE IN HUMAN PLASMA BY LIQUID LIQUID BY PLASMA HUMAN IN NATEGLINIDE OF DETERMINATION has been developed originally and validated for validated and originally developed been has (LC-MS/MS)method spectrometric mass tandem chromatographic liquid selective and sensitive CHROMATOGRAPHY TANDEM MASS SPECTROMETRY TANDEMMASS CHROMATOGRAPHY 1,* , Berrak GÜNEY International Symposium onDrugResearch &Development 2011 1Novagenix Bioanalytical DrugR&DCentre, Ankara, Türkiye 2Gazi University Faculty ofPharmacy, Ankara, Türkiye rd edition. Montvale, edition. 1 , SunaTOPTAN *[email protected] DRD 2011 P-047 102 - - 1 2. unteers. vol- healthy 36 in tablets nateglinide of study equivalence bio the to applied successfully was method this thermore, Fur-70°C. storedat when months for3.5 stable are samples plasma all that showedwere analyses Stability linearity. and selectivity precision, accuracy, the fulfills method The de. nateglini- for ng/mL 20000 – 50 of range the in linear was calibration the and ng/mL 50 quantitation of limit the with validated was method rate.The flow mL/min 0.3 and phase mobile as v/v/v) (700:300:0.9, acid acetonitrile:water:formic using with 30°C at column analytical ID) (2.1x50mm,3.5µm C18 Sunfire Waters a on performed was seperation raphic Chromatog- plasma. mL 0.5 with acetate ethyl using tion , SamiEREN Bauer S, Störmer E, Kirchheiner J et al. Rapid and simple and Rapid al. et J Kirchheiner E, Störmer S, Bauer Anal 31:551–555,2003. Biomed Pharm J detection. UV with analysis HPLC using plasma human in nateglinide of analysis the for method 1 , ErkinALKAN 1 , Tuncel ÖZDEN 2 - - POSTER PRESENTATIONS - In this study, albumin solution was treated with UV of the N-terminus of human albumin. 268:42–47, 2001. Eur J Biochem min binding and its potential as a marker for myocardial ischemia—a preliminary report. J Emerg Med 19: 311– 315, 2000. Bar-Or D, Lau E, Winkler JV. Novel assay for - cobalt-albu is known as albumin cobalt bonding (ACB) test recently ac cepted by [2-4]. FDA test ACB is based on the determination of a reduction in cobalt binding in the human serum albu- ischemia. during myocardial region min N-terminal light in the presence of titanium dioxide at different periods to produce ischemia modified albumin in vitro. Then cobalt chloride solution (2.32 mM) was incubated with UV light treated and untreated albumin solutions for 10 min. Unbound cobalt to albumin was determined using - voltam (100mM, pH 7.2), cobalt In buffer metric phosphate method. reduction peak was observed at -300 mV (vs Ag/AgCl) and at the scanning reverse the oxidation peak appeared at 540 mV (vs Ag/AgCl) potential while using cyclic voltammetry and mercury working drop electrode. 4. - - - - - 103 pro P-048 DRD 2011 DRD Rukiye DUMANLI, A. Nur ONAR DUMANLI, , Rukiye * *[email protected] Onur DUMANLI binding amino-acid residues 2+ International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International . It is produced in the in Itplasma. blood produced is and Ni 2+ human . Albumin comprises about half of the blood

55139 Samsun, Türkiye of Chemistry, Department of Science, Faculty Mayıs University, Ondokuz in in tein liver uman serum albumin is the most abundant

PRODUCTION OF ISCHEMIA MODIFIED ALBUMIN BY PHOTOCATALYSIS tion of the Co Denver, CO: Ischemia Technologies, August 2002. August Technologies, Ischemia CO: Denver, tory Medicine, second ed. Totowa, NJ: Humana, 2003. Totowa, tory ed. second Medicine, REFERENCES Several markers of ischemia have been proposed. The re The proposed. been have ischemia of markers Several Ischemia-modified albumin (IMA) is another biomarker The observation of serum albumin in patients with myo Bar-Or CurtisD, G, Rao N, Bampos N, Lau E. Characteriza - ACB Test Reagent Pack, COBAS MIRA Plus. Package insert. Package Plus. MIRA COBAS Pack, Reagent Test ACB Wu Wu AHB, editor. Clinical Markers: Pathology and - Labora H 3. 2. 1. serum protein. serum protein. with known clinical value in the assessment of patients pre search and development studies are underway to adequate to underway are studies development and search [1]. usefulness or lack of evidence their clinical ly validate with a suspected (ACS). coronarysenting acute syndrome cardial ischemia produced a lower metal binding capacity This albumin. normalserum nonischemic the than cobalt for POSTER PRESENTATIONS t a nt e edl asyd y UV-spectrophotometric by techniques. assayed readily be not can it chromophores, useful lacks primary memantine Since group. amine basic its of interaction ionic to due etc., chloride dansyl FMOC, like agent derivatization various to binding show may it that suggests 3.28), P (log lipophilic and 10.42) strated to beusefulindementia syndrome. ease and movement disorders. Recently, it has been demon- derivative rimantadine. Memantine is used in Parkinson’s dis- lated to the antiviral prototype amantadine and its α-methyl M Memantine free base, which is both highly basic (pKa (pKa basic highly both is which base, free Memantine 1 Anadolu University, HealthScience Institute, DepartmentofAnalytical Chemistry, 26470Eskişehir, Türkiye 2 Anadolu University, Faculty ofPharmacy, DepartmentofAnalytical Chemistry, 26470Eskişehir, Türkiye SPECTROPHOTOMETRIC DETERMINATION OF MEMANTINE MEMANTINE OF DETERMINATION SPECTROPHOTOMETRIC mn ceial ad hraooial re pharmacologically tricyclic and chemically a amine is hydrochloride) yladamantane - (1-amino-3,5-dimeth hydrochloride emantine HYDROCHLORIDE IN BULK FORM USING 4-CHLORO-7- USING FORM BULK IN HYDROCHLORIDE International Symposium onDrugResearch &Development 2011 NITROBENZOFURAZAN DERIVATIZATION NITROBENZOFURAZAN Neva ALASAĞ 1 DRD 2011 P-049 ,Dilek DOĞRUKOL AK 104 - .5 brt bfe slto b keig t t 70 at it keeping by solution buffer borate and M 0.05 (NBD-Cl) 4-chloro-7-nitrobenzofurazan 0.025M with gated. Memantine hydrochloride was succesfully derivatized investi- been have solvent dilution and acid, hydrochloric and agent derivatization of amounts the temperature, and time derivatization bufferpH, as such conditions perimental range of11.3–55.7µg/mLmemantine hydrochloride. concentration the over linear was method minutes. The 100 mum maxi- having spectrophotometry UV-vis by performed was yellowmemantinehydrochlorideof Determination product. a yield to 11.25 pH of buffer borate in (NBD-Cl) zofurazan - 4-chloro-7-nitroben with hydrochloride memantine of tion In In this study,

absorbance at 467 nm wavelength. nm 467 at absorbance

proposed method is based on the derivatiza- 2

The optimum ex optimum The o about C - POSTER PRESENTATIONS - - - 3 H C We have have We O . . N H Pseudomonas Pseudomonas O S O 3

Aouf N-acylsulfonamides 1, 2, 3 (Fig. (Fig. 3 2, 1, N-acylsulfonamides F were in prepared four steps car 3 H C O N H Nour-Eddine , Nour-Eddine * vitro are herein reported. Antibacterial activity S O O acylsulfonamides In our previous work, we have reported the synthesis synthesis the reported have we work, previous In our Zingaro Zingaro GJ, Siegel PKS, Kivlighn SD, Lotti VJ, Chang RSL, J Med Chem 37: 2263, 1994. WJ. Greenless 1990. 240, 33: Chem Med J J. Chang JM, Hand P, R. Carlson 2002. The The effects of these substitutions on biological ac Chang LL, WT, Flanagan KL, TB, Ashton Chen OMalley SS, Musser JH, Kreft Bender AF, RHW, Kubrak DM, Grimes D, Chem Soc Rev 8: 563, 1979. CW, Thornber Supuran CT, Scozzafava A, Clare, B. W. Med Res 22: 329, starting from Chlorosulfonyl Isocyanate (CSI) Isocyanate Chlorosulfonyl from starting N news series of modified modified of series news of of 1), 3. 4. 5. 6. established that CSI is a suitable reagent allowing the in the allowing reagent a suitable is CSI that established molecules. bioactive in moiety sulfonamides a troduction The acylation. and deprotection sulfamoylation, bamoylation, tivity in of these tree molecules was tested on . aureus and Staphylococcus , Escherichia Coli aeruginosa 2 - - - - 105 Figure 1 Figure erredjem N P-050 B DRD 2011 DRD or prote or *[email protected] 5 5 , Malika N-ACYLSULFONAMIDE 3 H C ouasla 1 O B , and antithyroid , and 4 N H , , antagonists for Angiotensin 2 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International O O S Radia N SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NOVEL activity among others. Another research research Another others. among activity 6

ubstituted ubstituted acylsulfonamides have been used as widely carboxylic acid bioisosteres in medicinal chemistry acidity1. their comparable due to

March DR, Mensah L, Nairn MR, O’Hanlon PJ, Oldham MD, MD, Oldham PJ, O’Hanlon MR, Nairn L, Mensah DR, March 10: 2263, 2000. Med Chem Lett Bioorg W. Yue 2006. (b) Connor E E. Sulfonamide Antibiotics Prim. Care Update Gyn Ob. 532, 1998. (c) Chambers, M S, Hobbs SC, Graham MI, Watt AP, Fletcher SR, Baker R, Fredman SB, Patel S, Smith AJ, Matassa VG. Bioorg Med Chem Lett 5: 2303, 1995. REFERENCES They They have received considerable attention due to Banwell Banwell MG, Crasto CF, Easton CJ, Forrest AK, Karoli T, (a) Yuan H, Silverman R B. Bioorg Med Chem 14: 1331, S Applied Organic Chemistry laboratory, Bioorganic Chemistry Group, University of Annaba, BP 12. Annaba. Algeria University of Annaba, BP 12. laboratory, Bioorganic Chemistry Group, Applied Organic Chemistry , leukotriene D4, receptors D4, , leukotriene 3 2. 1. tors tors or tRNA synthetases II activ antiviral with remarkable ent N-acylsulfonamides possess inhibitors HIV protease used clinically Some ity. structure. their in moiety sulfonamide a their their diverse biological activities, with several types of inhibi antibacterial possessing agents pharmacological ase ase inhibitory differ regards time last the in much progressed that line POSTER PRESENTATIONS clohexyl moiety clohexyl and p-chlorophenyl substituent on triazolo cy bearing compound the compounds, these Among [4]. various tested were compounds The 3. cylbromides phena- with stituted-2,4-dihydro-3H-1,2,4-triazol-3-thiones of reaction closure ring the via synthesized anaimprovedbroad spectrum safety profile2. their to owing infections fungal systemic of treatment the in role leading a play agents, antifungal triazole especially infections1. these treat to agents new for demand 2. 1. Sheehan DJ, Hitchcock CA, Sibley CM. Current and emerg - Candi- Invasive of Epidemiology DJ. Diekema MA, Pfaller n hs td, e tizltidaie derivatives triazolothiadiazine new study, this In 79, 1999. agents.antifungalazole ing 20(1):133-163,2007. Rev Microbiol Clin Problem. Health Public Persistent a diasis: REFERENCES T 1 Anadolu University, Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 26470Eskişehir, Türkiye Candida 2 is a rsle i a orsodn ices in increase corresponding a in resulted has to cies mainly due infections fungal life-threatening of incidence increased greatly he Zafer AsımKAPLANCIKLI Anadolu University, Faculty ofPharmacy, DepartmentofPharmacognosy, 26470Eskişehir, Türkiye pce aa oprd ih ketoconazole with compared ana species SYNTHESIS AND ANTICANDIDAL ACTIVITY OF NEW NEW OF ACTIVITY ANTICANDIDAL AND SYNTHESIS International Symposium onDrugResearch &Development 2011 TRIAZOLOTHIADIAZINE DERIVATIVES TRIAZOLOTHIADIAZINE Clin Microbiol Rev 12 (1): 40- (1): 12 Rev Microbiol Clin Ahmet ÖZDEMİR 1 , MehlikaDilek ALTINTOP 4-amino-5-sub n vitro in Candida *[email protected] against Azoles, DRD 2011 were P-051 spe 106 - - - - 1 , GökalpİŞCAN 4. 3. rophenyl substituent ontriazolothiadiazine ring. functional moieties, namely cycloaliphatic groupand p-chlo two ana activity candidal anti between correlation positive against derivative potent most the be to found was ring thiadiazine R Koneman EW, Allen SD, Janda WM, Schreckenberger PC, Schreckenberger WM, Janda SD, Allen EW, Koneman ZA, Kaplancıklı Turan-Zitouni G, Özdemir A, Revial G. New biology. USA:Lippincott-Raven Pub, 1997,p. 785-856. Micro Diagnostic Textbookand of Atlas Color WinnWC. antimicrobial agents. Eur Chem43:155-159,2008. JMed possible as derivatives triazolothiadiazine ana triazole AC 908. t s la ta tee s a is there that clear is It 90028). (ATCC albicans C. N 1,* , GülhanTURANZITOUNI N N 2 N R ' S R':NO H, R: 4-(OH)C R: 2 , F, Cl,F, , CH 6 H 1 5 , , C , 6 H 11 3 - - POSTER PRESENTATIONS , 1 , Cl, Br, F , Cl, Br, 2 ) 3 H O , N(CH 2 ) 3 R H O O O H N N Zafer Asım KAPLANCIKLI , Zafer 1 N CH CH( OH, , CN, 3 N N H N , OCH 3 , CH 2 2 REFERENCES Molecules 2007. 12: 1910-1939, derivatives. Rollas S, Küçükgüzel SG. Biological activities of hydrazone hydrazone of activities Biological SG. Küçükgüzel S, Rollas , Ahmet ÖZDEMİR R= NO R= 1. 1,* - - 107 P-052 DRD 2011 DRD Miriş DİKMEN DERIVATIVES [email protected] * Mehlika Dilek ALTINTOP Dilek , Mehlika 1 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Anadolu University, Faculty of Pharmacy, Department of Pharmacology, 26470 Eskişehir, Türkiye Eskişehir, 26470 Department of Pharmacology, of Pharmacy, Faculty Anadolu University, ydrazone ydrazone derivatives have attracted a great deal of interest in medicinal chemistry and - considera on ble them research in to their relation anti-pro 2

-MS spectroscopy. Anti-proliferative activity tests + Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskişehir, Türkiye 26470 Eskişehir, Chemistry, Department of Pharmaceutical of Pharmacy, Faculty Anadolu University, Gülhan Turan ZITOUNI Gülhan Turan

1 H SYNTHESIS AND ANTI-PROLIFERATIVE ACTIVITY OF SOME HYDRAZONE liferative liferative activity has been accomplished [1]. The structures of obtained compounds were confirmed by the spectrosco pic data of infrared (IR), nuclear magnetic resonance (NMR) and FAB were were performed on A549 (human lung cancer) Some cell compounds effective against were A549 (human lung lines. cancer) cell lines among these compounds. They exhibited time and dose dependent antiproliferative activity against line. cell A549 cancer POSTER PRESENTATIONS . Nanoparticles were SEM, bycharacterizedFTIR, techniqueNanoparticles 2,3. gelation pre polyelectrolyte Ionotropic by prepared were nanoparticles chitosan, of groups amine the and alginate of groups carboxyl between formation complex electrolyte poly the of Because alginate1. Sodium and Chitosan mers, biopoly mucoadhesive using Ofloxacin, drug antibacterial vitro in and formulation the describes work present The drops. eye an as eye the into instilled are those carriers natural of help 2. 1. ALGINATE/CHITOSAN NANOPARTICLES ACT AS A PROMISING SUSTAINED SUSTAINED PROMISING A ACTAS NANOPARTICLES ALGINATE/CHITOSAN Ludwig. Annick maceutics andBiopharmaceutics 65:10-17,2007. Phar of Journal European nanoparticles. nate/chitosan algi- into entrapment after structure insulin’ssecondary R. Antonio V, Francisco F, Domingos S, Bruno 57: 1595–1639,2005. Reviews Delivery delivery.AdvancedDrug drug ocular REFERENCES T Sankar RAJAVEL hrceiain f ptamc eiey ytm of system delivery ophthalmic of characterization the use of nanoparticle forming systems with the with systems forming nanoparticle of use the by drug ocular the of precornealelimination rapid and bioavailability ocular poor the overcome o

2 Faculty ofPharmacy, Dept.ofPharmaceutics, JSS College ofPharmacy, Ooty, Tamil Nadu,India 3 Faculty ofPharmacy, Dept.ofPharmacyPractice, SVCP, Thiruchengode,Tamil Nadu,India 1 Faculty ofPharmacy, Dept.ofPharmaceutics, ABIPER,Bangalore-64, Karnataka, India * Permanent address: 2/185Periyamanali Post. NamakkalDistrict. Tamil Nadu,India h ue f uodeie oyes in polymers mucoadhesive of use The RELEASE CARRIER FOR OCULAR DELIVERY OCULAR FOR CARRIER RELEASE International Symposium onDrugResearch &Development 2011 1,*,** , NagasamyVENKATESH ** [email protected] B. A.VISWANATH Probing DRD 2011 P-053 108 - - - 2 , K.GOWTHAMARAJAN 4. 3. frequency resultingfrequency better patient compliance. dosing reduced economical, more drops, eye conventional to alternative viable an was work developed the and stable and sterile more were nanoparticles optimized process.The showed that it follows first order release and fickian diffusion studies release vitro In drops4. eye conventionalophthalmic than hours 24 of period a over release sustained gradual a nanoparticles showed burst release at first hour then retained vitro 184.4nm. of size average an with nm 140-240 from size particle have nanoparticles loading. designed Drug The and

Sanjay KM, Shruti C, Sushma T, Kanchan K, Farhan JA, Roop

Pharmaceutics and Biopharmaceutics 68: 513–525, 2008. ain and zation Formulation,delivery:reservoirsocularscopicfor optimi KK Carbohydrate Polymers 74:813-821,2008. chitosan. and alginate using formation complex trolyte Heidi VS, Hilde KH, Hilde VS, Heidi release studies showed that chitosan/ sodium alginate sodium chitosan/ that showed studies release . Chitosan–sodiumalginate nanoparticles submicroas 1 in vitro in hrceiain Erpa Junl of Journal characterization. European Gjertrud M, Gjertrud 2 , M.P. NARMADHA Olav S,Bjorn TS. Polyelec TS.S,Bjorn Olav 3 , In - - - POSTER PRESENTATIONS - - doses or 80% vi- 50 values of cis-platinum, 50 compared compared to stilbene derivatives in aqueous and - nona Chem 50: 1213-1217, 2002. Food queous media. J Agric cytotoxicity and proliferation to survival: Application and J Immunol Methods 65: 55–63, 1983. assays. Mosmann, T. Rapid T. Mosmann, colorimetric assay for cellular growth ter ter combine drug The IC treatment. 3. ability doses of cis-platinum, viniferin and combined drugs, the early apoptotic rates of the combined drugs was deter showed results These alone. drugs of uses than higher mined that antioxidant reagent, viniferin would be able to reduce the dose but cytotoxic of this cis-platinum synergistically re agent showed antagonistic effect on lower doses that were test. isobologram by evaluated viniferin viniferin and combination of drugs 35 were µM, 130 µM and 16,25 mM (cis-platinum)-127,5 µM (viniferin), respectively. After the cells were treated with either IC - - 109 P-054 DRD 2011 DRD IN VITRO *[email protected] Mesut ŞEN, Zerrin İNCESU Mesut ŞEN, , Filiz ÖZDEMİR, * values were deter 50 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Gülşen AKALIN ÇİFTÇİ Gülşen

Türkiye Eskişehir, 26470 Department of Biochemistry, of Pharmacy, Faculty Anadolu University, is-platinum is-platinum is a widely used chemotherapeutic agent to treat malignant disease. Unfortunately, ototoxicity occurs in a large percentage of pa-

JP, Nepveu F. Antioxidant properties of trans-E-viniferin as trans-E-viniferin of properties Antioxidant F. Nepveu JP, nisms of cisplatin-induced ototoxicity and prevention. 226: 157–167, 2007. Hearing Research REFERENCES Privat C, Telo JP, Bernardes-Genisson V, Vieira A, Souchard Souchard A, Vieira V, Bernardes-Genisson JP, Telo C, Privat Leonard Leonard PR, Craig Debashree AW, M, Vickram R. Mecha- C COMBINATION EFFECTS OF CIS-PLATINUM AND VINIFERIN FOR GLIOMA cies (ROS), which can trigger cell 1. death In this regard, we aimed to investigate combination effects of cis-platinum and viniferin, which is an 2 antioxidant, on glioma (C6) cells. Here, cytotoxic activities of both drugs against the C6 cells were assessed using MTT 3. The assay IC tients tients treated with higher dose regimens. The mechanisms appear to involve the production of reactive oxygen spe mined. mined. Apoptotic cell ratio was investigated by annexin-V/ propidium iodide by flow cytometer (Becton-Dickinson) af- 2. 1. POSTER PRESENTATIONS 2. 1. n sm dmntae atmcoil s el s biofilm as well as antimicrobial demonstrated some and antioxidant higher showed esters aromatic synthetic the of the Majority mold. and yeasts inhibit bacteria, positive Gram of growth to found were compounds Some side. FA on group hydroxyl phenolic free bearing compounds in found only was capacity scavengingradical α-tocopherol.DPPH of that than activity better FAor of equally derivativesshowed ester aromatic all of capacity scavenging radical superoxide in activities antimicrobial and tial potenscavenging- radicalantioxidant, their tested are cules mole laboratory.These our in synthesized been have lated acety or free was FA of hydroxyl phenolic the which in FA SYNTHESIS AND BIOLOGICAL EVALUATION OF SIMPLE AROMATIC ESTERS ESTERS AROMATIC SIMPLE EVALUATION OF BIOLOGICAL AND SYNTHESIS aicae R Snhss n eauto o cfec acid caffeic of evaluation and Synthesis R. Padinchare, Çalışkan, B. et al., Synthesis, antioxidant and antimicrobial 217, 2001. 215- 11: Lett Chem Bioorg&Med antioxidants. as amides 2010,inpublication.Pharm Res evaluation of simple aromatic esters of ferulic acid. Archiv REFERENCES T Şeyma CANKARA PİROL Therefore, a series of aromatic ester derivatives of derivatives ester aromatic of series Therefore,a establisted. well is plants in derivatives ester alkyl its and (FA) acid ferulic of activity antioxidant he AND AMIDES OF SOME HYDROXYCINNAMIC ACIDS HYDROXYCINNAMIC SOME OF AMIDES AND International Symposium onDrugResearch &Development 2011 2Pharmaceutical Microbiology, Faculty ofPharmacy, test systems. The systems. test vitro in Gazi University, 06330Etiler, Ankara, Türkiye 1Departments ofPharmaceutical Chemistry 1, * , Burcu ÇALIŞKAN *[email protected] DRD 2011 P-055 110 - - 4. 3. microbial activities. anti - their investigate FAto of derivatives amide piperazine and ester various prepared have we information, above on Based 2-4. activity anticancer and antioxidant antimicrobial, have to reported been have acid caffeic of derivatives ide am- some Meanwhile, FA1. of that than activity eradication of FA. General structure of synthesized ester and amide derivatives Jie, F. Synthesis, structure and structure-activity relation- structure-activity and F.Jie, structure Synthesis, ogi, . ytei, ilgcl vlain n struc and evaluation biological Synthesis, Z. Hongbin, crobials. Eur Chem45:2638-2643,2010. JMed antimi - potential as amides acid caffeic of analysis ship 6351- 6359, 2010. 18: Chem Bioorg&Med derivatives. acid caffeic aza- cytotoxic novel of study relationship ture-activity 1 , Fatma KAYNAK 2 , Erden BANOĞLU 1 - POSTER PRESENTATIONS

- - * In the effort to get those agents, herein, we have report Pharm Pharm Med Pharm Pharm Chem 337: 281- 288, 2004. Arzneimittel derivatives. acid kojic new of activity vulsant 60(1): 22–29, 2010. Forschung chlorokojic acid derivatives with their antimicrobial and J Med activities. Chem 45: 4089-4095, 2010. Eur antiviral ties of new Mannich bases of chlorokojic 10.1007/ DOI: manuscript (accepted Res Chem Med acid tives. deriva- s00044-010-9338-x). Aytemir Aytemir MD, Septioğlu E, Çalış Ü. Synthesis and - anticon Aytemir MD, Özçelik B. A study of cytotoxicity of novel Aytemir MD, Özçelik B. Synthesis and biological activi- ed several new 6-hydroxymethyl-3-hydroxy-2-substituted 4H-pyran-4-one derivatives including benzyl and halogen 3,4-dichlo 4-chloro, 3-chloro, as such derivatives substituted ro and 2,6-dichloro. The structures of the compounds were using IR and ESI-MS data. by identified allomaltol allomaltol H-pyran-4-one) (5-hydroxy-2-methyl-4 were syn- were activities biological their and laboratory our in thesized These evaluated. compounds found to have remarkable an- 4-7. effects and anticonvulsant antiviral timicrobial, 5. 6. 7. 111 P-056 DRD 2011 DRD *[email protected] Mutlu D. AYTEMİR , Mutlu D. KARAKAYA Gülşah International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

SYNTHESIS OF SOME NOVEL MANNICH BASES OF KOJIC ACID ojic acid H-pyran- (5-hydroxy-2-hydroxymethyl-4 4-one) is a natural fungal metabolite by produced many species of Aspergillus and Penicillium

Since Since the physicochemical properties of kojic acid is anticonvulsant anticonvulsant and antimicrobial activities of 3-hydroxy- 4H-pyran-4-one 6-methyl-2-substituted Arch derivatives. Kojic acid and its derivatives: History and present state of Historystate derivatives: present its and and acid Kojic 2004. Health 12: 16–18, J Publ art. Eur Cent pects of Pharm kojic 33: acid 80-101, in Toxic Regulfood. 2001. century of science for kojic acid. Nat Prod Rep 23: 1046- 1062, 2006. REFERENCES Aytemir MD, Çalış Ü, Özalp M. Synthesis and evaluation of evaluation and Synthesis M. Özalp Ü, Çalış MD, Aytemir Brtko J, Rondahl L, Fickova M, Hudecova D, Eybl V, Uher M. Uher V, Eybl D, Hudecova M, Fickova L, Rondahl J, Brtko Burdock GA, Soni MG, Carabin IG. Evaluation of health as- health of Evaluation IG. Carabin MG, Soni GA, Burdock Bentley R. From miso, sak´e and shoyu to cosmetics: A K Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06100 Sıhhiye, Ankara, Türkiye Türkiye Ankara, Sıhhiye, 06100 Chemistry, of Pharmaceutical Department of Pharmacy, Faculty University, Hacettepe suitable, suitable, a reasonable number of derivatives of kojic acid has been prepared so far. Halogen derivatives of kojic acid including chlorokojic acid H- (5-hydroxy-2-chloromethyl-4 pyran-4-one) which is synthesized by chlorination of kojic acid has significant antibacterial and antifungal activities3. Mannich bases Previously, of kojic acid, chlorokojic acid and moulds1. Due to its tyrosinase inhibitor activity, it has been ad- food a and cosmetic in agent skin-whitening a as studied ditive to prevent enzymatic browning. Kojic acid has been used been has it addition, In antioxidant. an as food to added and analytical chemical2. pesticide, as an antibiotic, 4. 3. 2. 1. POSTER PRESENTATIONS Turkey.B Compounds University, Osmangazi Eskişehir the of Experimentation mal haveapprovedbeen Localbythe CommitteeEthical Ani - on kg) was used as a standard drug. The experimental protocols mg/ 3 and mg/kg (1 Donepezil tests. cage activity of cation appli- the with examined were rats of activities locomotor spontaneous on compounds test of Effects rats. in SMAD of 5 mg/kg and 10 mg/kg) on learning and memory parameters ordertestin of compoundsmg/kg,toeffects (1 examinethe performed was test avoidance and Active bilaterally. days, third first at mg/kg) (3 STZ of injection cerebroventricular intra- by generated was SMAD analyses. spectral Mass and the synthesized compounds were elucidated by IR, by elucidated were compounds synthesized the of Structures [1-3]. sabeluzol and FK960 donepezil, agents, anti-Alzheimer of groups com - functional on based were test pounds of Syntheses rats. in (SMAD) disease zheimer’s

2. 1. LEARNING AND MEMORY PARAMETERS OF STREPTOZOTOCIN MODEL OF OF MODEL STREPTOZOTOCIN OF PARAMETERS MEMORY AND LEARNING THE EFFECTS OF SOME BENZOTHIAZOLE/PIPERAZINE DERIVATIVES ON ON DERIVATIVES BENZOTHIAZOLE/PIPERAZINE SOME OF EFFECTS THE I Mohr E, Nair NP, Sampson M, Murtha S, Belanger G, Pap G, Belanger S, NP,Murtha Nair M, E, Sampson Mohr MD.Alzheimer’sPeskind R, MD,Elaine Raskind A, Murray pas B, Mendis T. Treatment of Alzheimer’s disease with sa- 85: 803-817, 2001. Am North Clin Med disorders. related and disease REFERENCES 2 Anadolu University, Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 26470Eskişehir, Türkiye netgtd sn srpoooi (T) oe o Al- of model (STZ) streptozotocin using investigated were parameters memory and learning on derivatives benzothiazole/piperazine five of effects study, this n 1 Anadolu University, Faculty ofPharmacy, DepartmentofPharmacology, 26470Eskişehir, Türkiye Ümide DEMİRÖZKAY ALZHEIMER’S DISEASE IN ACTIVE AVOIDANCE TEST AVOIDANCE ACTIVE IN DISEASE ALZHEIMER’S 2 -B 3 at 10 mg/kg and B and mg/kg 10 at International Symposium onDrugResearch &Development 2011 1 4 , Yusuf ÖZKAY -B 5 at 5 and 10 and 5 at * [email protected] 1 H-NMR DRD 2011 P-057 112 - 2,* in rats. SMAD of deficits memory and learning the to related eters ies revealed that, four of the compounds repaired the param- spontaneous locomotor of activities rats. Experimental stud- the changed significantly not were compounds test the of Any donepezil. of doses mg/kg 3 and mg/kg 1 as effective as were doses mg/kg 10 and 5 at B4-B5 doses, mg/kg 10 at zyl, B zyl, R: B on B pound Com- rats. of responses avoidance of number the increased mg/kg doses significantly decreased the latency periods and 3. , Yusuf ÖZTÜRK Doggrell SA. The potential of activation of somatostatin- of activation of potential SA. The Doggrell ease. Expert OpinInvestigease. Drugs13:69-72,2004. Expert dis- Alzheimer’s in FK960 with neurotransmission ergic ropharmacol 20:338-345,1997 Neu- Clin correlates. structural and Functional beluzole: 1 ; Phenyl, B 5; 4-Chlorobenzyl 1 a fud o e nfetv. opud B2-B3 Compounds ineffective. be to found was 2; Benzyl, Benzyl, B N S 1 , İlhanIŞIKDAĞ 3; 4-Methoxybenzyl, 4-Methoxybenzyl, B H N O N 2 4; 4-Methylben- N R POSTER PRESENTATIONS e l o z a ) z n e 2 (B S O N , İlhan IŞIKDAĞ 2 N O effects of 2-(2-carboxyphenylsulfanyl)-N-(4-substituted phenyl)acetamide derivatives. Med Chem Res 20: 152- 157, 2011. Özkay-Demir Ü, Özkay Y, Can ÖD, Synthesis and analgesic and Synthesis ÖD, Can Y, Özkay Ü, Özkay-Demir spectral analyses. MTT assay was applied for determination of cytotoxicity levels of the compounds. The compounds 7 and 9 found to be and most C6 cytotoxic on cell lines, HT-29 respectively. 2. - - Nur İpek ÖNDER , Nur İpek 2 113 P-058 DRD 2011 DRD [email protected] * , Zerrin İNCESU 1,* International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Yusuf ÖZKAY Yusuf ANTICANCER ACTIVITY OF SOME ISOXAZOLE DERIVATIVES

Anadolu University, Faculty of Pharmacy, Department of Biochemistry, 26470 Eskişehir, Türkiye Eskişehir, 26470 Department of Biochemistry, of Pharmacy, Faculty Anadolu University, 2 s we reported previously, azole and benzazole derivatives possess chemotherapeutic impor 1. tance Hence, in the present study some - isoxa

Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskişehir, Türkiye 26470 Eskişehir, Chemistry, of Pharmaceutical Department of Pharmacy, Faculty Anadolu University, 1 REFERENCES stituted-N-[4-(1-methyl-4,5- stituted-N-[4-(1-methyl-4,5- H-imidazole-2-yl) diphenyl-1 phenyl]acetamide derivatives and evaluation of J Med Chem 45: 3320-3328, 2010. Eur activity. anticancer their

Özkay, Y, Işıkdağ İ, Y, İncesu Özkay, Z, Akalın G. Synthesis of 2-sub A 1. zole derivatives bearing zole derivatives azoles and benzazoles as imidazole, triazole, tetrazole, thiadiazole, benzimidazole and - benzothi cytotoxic their investigate to order in synthesized were azole activity on C6 (glioma) and HT-29 (colon cancer) cell lines. Target compounds were synthesized in accordance our with reported 2. method Reaction of various mercapto-(benz) azoles and 3-(2-chloroacetamino)-5-methylisoxazole gave the 3-[2-substitutedsulfanylacetamino)-5-methylisoxazole by elucidated were compounds the of Structures derivatives. POSTER PRESENTATIONS Structures of the compounds were elucidated by spectral spectral by elucidated were compounds the of Structures derivatives. 2-chloro-1,2-diaryl-ethanone with acid ylacetic - 4-thioureido-phen reacting by ethanol in performed were sic and anti-inflammatory activities. Synthesis of compounds analge possible their investigate to as so synthesized were derivatives acid acetic phenyl based thiazole novel some of nonsteroidal anti-inflammatory agents. Thus, in this study, class a constitute diclofenac and ketorolac,etodolac, lindac, su- indomethacin, as such derivatives acid acetic Aryl [1-3]. compounds based thiazole of effects anti-inflammatory and 2. 1. Franklin PX, Pillai AD, Rathod PD, Yerande S, Nivsarkar Nivsarkar S, Yerande PD, Rathod AD, Pillai PX, Franklin Pancholi SC, Chaturvedi KK, FP,Vasu Xavier RN, Sharma M, Padh H, Vasu KK, Sudarsanam V. 2-Amino-5-thiazolyl 2-Amino-5-thiazolyl V. Sudarsanam KK, Vasu H, Padh M, 890-897, 2009. 24: Chem Med Inhib Enzyme J approach. design drug analogue-based an as agents: anti-inflammatory potential derivatives 4-benzyl-1,3-thiazole of Synthesis SS. REFERENCES T 1 Anadolu University, Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 26470Eskişehir, Türkiye ANALGESIC AND ANTIINFLAMATORY ACTIVITY OF SOME THIAZOLE THIAZOLE SOME OF ACTIVITY ANTIINFLAMATORY AND ANALGESIC e. hr ae oe eot icuig analgesic including reports some are There ies. stud- development drug new to subjected often is which ring hetorocylic important an is hiazole 2 Anadolu University, Faculty ofPharmacy, DepartmentofPharmacology, 26470Eskişehir, Türkiye Yusuf ÖZKAY International Symposium onDrugResearch &Development 2011 1,* , ÖzgürDevrim CAN * [email protected] DERIVATIVES DRD 2011 P-059 2 114 , ÜmideDEMİRÖZKAY - ferent extents. dif- to activities anti-inflammatory and compounds analgesic exhibited synthesized that revealed tests macological Phar respectively. activities, anti-inflammatory and algesic an- observe to out carried were tests edema paw induced analyses. Acetic acid-induced writhing test and carrageenan- R: Various substituents 3. R R Nagatomi H, Ando K. Studies on the anti-inflammatory anti-inflammatory the on Studies K. Ando H, Nagatomi tives. Arzneimittelforschung 34:599-603,1984. deriva- acid 2-amino-thiazoleacetic especially rivatives, de thiazole of effect adverse ulcerogenic and activity 134, 2008. 129- 43: Chem Med J Eur structures. diverse of agents anti-inflammatory designing for scaffold novel A motif: N S H N 2 , Leyla YURTTAŞ 1 C O O H - - POSTER PRESENTATIONS - - - - = 2 1 0.73 and Q

= 2 This This work was financially sup scaffold. Depending on the negative Mükerrem Betül YERER , Mükerrem 2 Acknowledgement: Acknowledgement: It was found that the -log (IC50) values of the compounds compounds the of values (IC50) -log the that found was It a series of 4-anilino quinazoline derivatives as tyrosine kinase (EGFR) inhibitor: An approach to design - antican Biostruc and Nanomaterials of Journal Digest agents. cer 2: 387-40, 2010. tures Malleshappa NN, Harun MP, Varun B. 2D B. QSAR studies Varun on Malleshappa NN, Harun MP, ported by Erciyes University Scientific Research - Proj No; FBD-10-2983). (Grant Turkey ects (BAP) of 0.68). static static character of the substituents at seven positions of the 4-Anilino Quinazoline these in embedded correctly groups the of charge positive or substituents, the 3D bio-structure to increase or decrease set test A predicted. was set training the in values (IC50) -log of fourteen compounds was used to evaluate the predictiv ity of the model. Although only atomic properties defined through topological descriptors were used in the calcula- MCET4D-QSAR the resulting from the model activity, of tion method was of sufficient statistical quality (R were were highly dependent on the topology, size and electro 2. - - - 115 P-060 DRD 2011 DRD Gökçe ALTIPARMAK , Gökçe INHIBITORS Relation- 2 [email protected] * Activity Yahya GÜZEL , Yahya 1, * Erciyes University, Faculty of Pharmacy, 38039 Kayseri, Türkiye of Pharmacy, Faculty University, Erciyes 1 We attempt to find re consistent We International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International 1,2. Erciyes University, Faculty of Science, Department of Chemistry, 38039 Kayseri, Türkiye of Chemistry, Department of Science, Faculty University, Erciyes 2 inhibitors inhibitors Epidermal Growth Factor Receptor

SAR Structure uantitative- (Q Ships) is one of the various cheminformatic ap proaches proaches possible for efficient model building. Hayriye YILMAZ Hayriye

PHARMACOPHORE AND FUNCTIONAL GROUP IDENTIFICATION OF 4-ANILINO QUINAZOLINE AS DERIVATES TYROSINE KINASE (EGFR) tyrosine tyrosine kinase inhibitors. Chem. Rev 101: 2001. 2573-2600, REFERENCES A 4D QSAR analysis was applied to a series of 61 4-Anilino 4-Anilino 61 of series a to applied was analysis QSAR 4D A

Kurup Kurup A. Garg R. Hansch C. Comparative QSAR study of Q Figure 1. Structure of 4-(X-bromoanilino)-Y-quinazolines. Figure 1. Concisely, QSAR is a mathematical equation relating molecu- relating equation mathematical a is QSAR Concisely, activity biological known - to series descriptors com lar of for pounds so that this model can be used to evaluate activity of new chemical entities (EGFR) by the MCET (EGFR) by method. Quinazoline lationships lationships between the values of molecular properties and the biological activity, and try to rationalize the structure- activity relationship using Molecular Comparative Electron (MCET)Topologic method. In four dimensional quantitative structure activity relationship (4D QSAR) analyses, the activ which via atoms ityaccurately much more can be calculated conformers. the defined positions of the align at located are POSTER PRESENTATIONS 2 oeue o Nbnypprdn drvts I odr to order In derivates. N-benzylpiperidine of molecules 82 of series a for it applied have and us, by developed newly is which method, (MCET) topological electron molecular conformer called method computational a used have we AChE, of activity inhibitory predict and requirements tural struc understand to order in So conformers. the of matrix the comparing performed is analyses QSAR) (4D tionship rela- activity structure quantitative dimensional four study this In expression. mathematical a into properties their and molecules of structure the between relationship the dense con- to is modeling Relationship) Activity Structure titative (Quan - QSAR of strategy AD.The of treatment the to cation appli- for candidates appropriate them makes level toxicity low a with activity inhibitory AChE high a of combination A acetylcholinesterase(AChE). of inhibitors selective and tent N-benzylpiperidine derivates are competitive, reversible, po systems1. cholinergic and dopaminergic serotoninergic, e.g. neurotransmission, of deregulation the by biochemically and loss memory a by clinically itself manifests pathology 1. LIGAND BASED RESEARCH OF 82 OF RESEARCH BASED LIGAND A Bernard P, Kireev DB, Chrétien JR, Fortier PL, Coppet L,. Coppet PL, Fortier JR, Chrétien DB, P,Kireev Bernard to Mouse acetylcholinesterase and comparativemolecu- and acetylcholinesterase Mouse to Automated of docking 82 derivativesN-benzylpiperidine REFERENCES Hayriye YILMAZ motn pr o te lel pplto. This population. elderly the of part important increasingly an affecting disease degenerative zemrs ies (D i a rgesv neuro progressive a is (AD) disease lzheimer’s MOUSE ACETYLCHOLINESTERASE AND 4D QSAR ANALYSIS QSAR 4D AND ACETYLCHOLINESTERASE MOUSE 2 Erciyes University, Faculty ofScience, DepartmentofChemistry, 38039Kayseri,Türkiye International Symposium onDrugResearch &Development 2011 1,*

1 Erciyes University, Faculty ofPharmacy, 38039Kayseri,Türkiye , Gökçe ALTIPARMAK * [email protected] DRD 2011 P-061 N- 2 116 , Yahya GÜZEL - - - BENZYLPIPERIDINE DERIVATIVES TO DERIVATIVES BENZYLPIPERIDINE BITAK) (Grant No: TBAG-108t148). ed by the Scientific Technical Research Council of Turkey- (TU similar ordifferent skeleton. of molecules the for activity inhibitory AChE in decrease or increase an either to lead that interactions ligand-receptor benzylpiperidine group.(APS)N- shielding macophoreincluding analysis This of pharmacophore group (Pha), auxiliary (AG) and anti-phar identificationfor detail in used.described are is method The method MCET in (GA) algorithm genetic and (PLS) squares find the more convenient set of descriptors, least-the partial Acknowledgement: puter-Aided Design 13:355-371,1999. Molecular analysisfield lar with ‘natural’alignment. Comof Journal - Figure 1. 2 , Burçin KILIÇ molecules is used to obtain information on

N-Benzylpiperidine derivatives. N-Benzylpiperidine This study was financially support financially was study This 2 , Zülbiye ÖNAL 2 - - POSTER PRESENTATIONS - - 2 Sefa AKSAKAL , Sefa 2 oluble oligomers from a non-disease related protein STJ. F G, Ferreira Martinez J C, De Felice A M, Houzel S mimic Abeta-induced tau hyperphosphorylation 2: 736-748, 2007. . Neurochem neurodegeneration and ing of conformation space for both cyclic and acyclic mole cal- dynamics molecular and minimizations energy After cules. culations are performed the acceptable state conformers of the crucial most The selected. are molecule each for energy lowest step in performing 4D-QSAR is to determine the bio-structure - an and (AG) group auxiliary (Pha), pharmacophere by formed tipharmacophere shielding (APS) so that all compounds could in conformers molecular using By Pha. via together aligned be MCET method, we attempted 4D-QSAR study.As biological activities are generally skewed, the reported IC50 values were (par PLS usual, As logIC50. corresponding the into converted tial least squares) method was used to establish and validate 4D-QSAR, and LOO (leave-one-out) cross-validation method The was used cross-validated co- to evaluate the initial model. efficient q2 was calculated, the optimum number of components was then given, and the 3D model, consist of Pha, AG and APS was finally derived corresponding to the optimum number.The results are listed, and the graphic results for the experimental versus predicted activities of both training set The and good test agreement between set actual are displayed. and predicted logIC50 values for the test set compounds suggests that the constructed 4D QSAR models are reliable and inhibitors.v aggregation tau novel of design the for used be can Zülbiye ÖNAL , Zülbiye 2 - - 117 P-062 DRD 2011 DRD [email protected] * Yahya GÜZEL , Yahya 1,* Erciyes University, Faculty of Pharmacy, 38039 Kayseri, Türkiye of Pharmacy, Faculty University, Erciyes

1 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International 4D QSAR STUDYING WITH MCET METHOD ON

Hayriye YILMAZ Hayriye PHENYLTHIAZOLYLHYDRAZIDE (PTH) DERIVATIVES

Erciyes University, Faculty of Science, Department of Chemistry, 38039 Kayseri, Türkiye of Chemistry, Department of Science, Faculty University, Erciyes 2 he pathological hallmarks of Alzheimer’s disease (AD) are two types of aggregates in brain: extracellular amyloid plaques consisting of the Aβ T Vieira Vieira MN, Forny-Germano L, Saraiva LM, Sebollela A, - therapeu to road the on problems and progress disease: Science 297: 353-6, 2002. tics. REFERENCES In this we study, report a 4D-QSAR study on the PTH de In respect to the molecular conformations, quantum

Hardy J, Selkoe DJ. The amyloid hypothesis of Alzheimer’s Alzheimer’s of hypothesis amyloid The DJ. Selkoe J, Hardy 2. 1. peptide[1] and intracellular neurofibrillary tangles (NFTs). [2] Abnormal filaments called helical paired filaments (PHFs) are major components of NFTs, and a microtubule- associ- ated protein tau consists of its core protein. Even though the primary cause of these aggregation processes in well-understood, there not is a general consensus that protein series of pathological a and neurons for toxic are aggregates AD. finally and neurodegeneration to lead events neurotoxic chemical calculations are obtained via “Spartan’08” software “Spartan’08” chemical calculations are obtained via program. In the first step, Spartan’s molecular mechanics forcefield (MMFF) is used, because it presently provides the calculation of equilibrium geometries, strain energies and normal-mode vibrational frequencies, as well as for - search rivatives rivatives in anticipation of getting a model that would ac count for the quantitative differences in bioactivity seen in this series and provide insights into designing of novel tau activity. improved with inhibitors aggregation POSTER PRESENTATIONS plant based coumpounds has long been a source of medici- sourceof a been long has coumpounds based plant The infections2,3. eye related lenses contact with associated Moreover QS1. via formation biofilm and protease) (elastase, factors virulence of production controls aeruginosa Pseudomonas (QS). sensing quorum called process a in regulation gene 2. 1. CINNAMALDEHYDE INHIBITS BIOFILM FORMATION ON CONTACT ON FORMATION LENSES BIOFILM INHIBITS CINNAMALDEHYDE M Szczotka-Flynn LB, Pearlman E, Ghannoum M. Microbial Microbial M. Ghannoum E, Pearlman LB, Szczotka-Flynn patho the and biofilms Bacterial JS. Kilty D, Al-Mutairi 2:116-129, 2010. their accessories: A Literature Rewiev. Eye & Contact Lens and solutions,care lens lenses, contact of contamination Allergy 11:18-23,2011. andClinicalImmunology in Opinion Current rhinosinusitis. chronic of physiology REFERENCES is one of the most common bacteria bacteria common most P.the of one is aeruginosa 2 Department of hi on ouain est ad coordinate and density population monitor own their to molecules signal lactone serine use bacteria negative Gram any 1 Ebru ÖNEM Department ofBiology, Suleyman Demirel University, 32260Isparta, Türkiye International Symposium onDrugResearch &Development 2011

Clinical Microbiology, Faculty ofMedicine,Marmara University, İstanbul, Türkiye 1, * , Seyhan ULUSOY -acyl homo N-acyl * [email protected] DRD 2011 P-063 118 - - 1 , GülgünBOŞGELMEZTINA 4. 3. on biofilmformation low concentration. at very activity inhibitor significant showed was Cinnamaldehyde assay. violet crystal with lenses contact on cinnamaldehyde against vestigated infections.ment ofbacterial treat the in interest great been has compounds natural of nes4. As much as their antibacterial effect, anti-QS properties Cragg GM, Newman DJ, Snader KM. Natural products products Natural KM. Snader DJ, Newman GM, Cragg Fraunholz B, Giese AJ, McBain R, Matthes C, Rändler 1997. in drug discovery and development. J Nat Prod 60: 52-60, lenses.gel contact 10:282,2010. BMCMicrobiology hydro upon formation biofilm and adhesion aeruginosa studying for system in-vitro three-phase A A. Kramer and No Hübner T, Kohlmann , R Sietmann M, In this study, the inhibition of biofilm formation was in- was formation biofilm of inhibition the study, this In A1 n h peec of presence the in PAO1 aeruginosa P. 1,2 Pseudomonas - - POSTER PRESENTATIONS - - - - . 5 6(6): 456-463, N H N N C O 2 H H C N C N ux l ef r A , r 4 19(4): 409-428, 1978. 409-428, 19(4): SO

2 3, * 2 H conc. H N b) H ., ( .t N o r

t C O c) ( H N F, 4 °C M , Ünsal ÇALIŞ As a result of activityof of result a napthtylAs while studies; derivative This project is supported by Hacettepe University Scien - oric model studies. Lett Drug Des Discov 2009. JP. Synthesis of an their and some derivatives ether oxime and oxime ethanone 1-(2-naphthyl)-2-(imidazole-1-yl) ticonvulsant and activities. antimicrobial Eur J Med Chem ticonvulsant 2001. 36(5): 421-433, May Drug Drug 2. Antiepileptic Development. Anticonvulsant Epilepsia Screening. Karakurt Karakurt A, Dalkara S, Özalp M, Özbey S, Kendi E, Stables Krall Krall RL, Penry JK, EA. White HJ, BG, Swinyard Kupferberg D a)

1, 2 ( : semicarbazones semicarbazones showed protection against all tested doses any showed not derivative biphenyl test, MES at h 0.5 except neurotoxic any shown not have structures two Both activity. doses. ity all tested at No: 07 01 301 002. Project Unit. tific Research 4. 5. techniques such as IR, NMR, ESI-MS and HRMS. Anticonvulsant Anticonvulsant HRMS. and ESI-MS NMR, IR, as such techniques maxi by standarts reference against examined were activities pentylenetetrazol (MES) and mal subcutaneous electroshock (scPTZ) was induced seizure tests. Neurotoxicity determined in performed were tests these All test. toxicity by the rotorod De Drug Antiepileptic the of procedures the with accordance National by developed was which program (ADD) velopment (NINDS) Stroke and Disorders Neurological of Institute s - - - eagent 119 R N P-064 ) DRD 2011 DRD 18(9): 18(9): l

y 1- N - 2 H [email protected] Sıhhiye-Ankara, Türkiye Sıhhiye-Ankara, * pheny C i B C O 4- ( - r A , 1,1' l hy Ebubekir SEPTİOĞLU Ebubekir apht N N 2- -imidazole-1-yl)-1-aryl -imidazole-1-yl)-1-aryl eth a) = ( H r N A H International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International r B Schematic representation and structures of synthesized compounds. and structures of synthesized Scheme: Schematic representation 2 H new antiepileptic agents which is more C C O r

A reparing active and has less toxicity is one of the studies current on development of biologically active SYNTHESIS AND ANTICONVULSANT OF EVALUATION SOME NEW Kavacık Pharmacy, Kavacıksubayevleri Mah. Sandalcı Sok. No: 20/B-C 06120 Keçiören-Ankara/Türkiye Mah. Sandalcı Kavacıksubayevleri Pharmacy, Kavacık

2 On Leave from Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 University, Hacettepe of Pharmacy, Faculty Chemistry, Department of Pharmaceutical from On Leave PHENYLSEMICARBAZONE DERIVATIVES OF ARYLALKYLIMIDAZOLES 1 Epilepsy Res 45(1-3): 3-6, 2001. REFERENCES ni V, Afarinesh M. Synthesis and anticonvulsant activity of activity and M. anticonvulsant ni Synthesis V, Afarinesh Res Chem Med 4-(2-phenoxyphenyl)semicarbazones. A A series of some novel 2-(1 ticonvulsant activity of a novel series of 2,5-disubstitutedof series activitynovel a of ticonvulsant 1,3,4-oxadiazoles: Semicarbazones based - pharmacoph 758-769, 2009. 758-769, Shafiee A, Rineh A, Kebriaeezadeh A, Foroumadi A, Sheiba A, Foroumadi A, Kebriaeezadeh A, Rineh A, Shafiee Brodie MJ. Do we need any more new antiepileptic drugs? antiepileptic new more any need we Do MJ. Brodie

- An P. Mishra Kharya MD, P, Singour R, Veerasamy H, Rajak P

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 Sıhhiye-Ankara, Türkiye Türkiye 06100 Sıhhiye-Ankara, University, Hacettepe of Pharmacy, Faculty Chemistry, Department of Pharmaceutical 3 2. 1. arylalkylimidazoles have anticonvulsive arylalkylimidazoles effects 4. too In anticonvulsive hope have of getting synergistic response by gathering semicarbazone this in structure, same the at arylakylimidazolefunctions and study we prepared two new compounds and evaluate their activities. anticonvulsant drugs1. Recently, the anticonvulsant activities of semicarbazone derivatives were reported by various studies2,3. Also 3. ane-1-one ane-1-one N-phenylsemicarbazones were synthesized and with 1-ar by the of prepared reaction phenylsemicarbazides to evaluate yl-2-imidazol-1-yl-ethanone their anticonvulsant were compounds of the synthesized structures The activities. spectroscopic the and results analysis elemental by confirmed POSTER PRESENTATIONS structure infections,structure andsexually transmitted diseases2. skin and skin infections, tract respiratory lower and upper treattobacterial used also is It bacteriostatic. or bactericidal be may synthesisdrugs 1. proteinThesesuppresses and teria is designed in a special way to withstand against high sys- high against withstand to way special a in designed is system chromatographic UPLC consumption. solvent and time of decrease chro with concerning liquid especially in matography, possibilities new giving technique new a 2. 1. DEVELOPMENT AND VALIDATION OF UPLC METHOD FOR DETERMINATION DETERMINATION FOR METHOD UPLC VALIDATION OF AND DEVELOPMENT A

erpuo A, ovl E, trsa L Wlo DN, Wilson AL, Starosta EC, Kouvela AD, Petropoulos mechanisms and Characteristics DL. Hand HW, Lee lr Promne iud hoaorpy UL) is (UPLC) Chromatography Liquid Performance Ultra romycin to Escherichia coli ribosomes. J Molecular Molecular J ribosomes. coli Escherichia to romycin azith- of binding Time-resolved DL. Kalpaxis GP, Dinos Antimicrobial J Agents 18:419-425, 2001. Int human leukocytes. in efflux polymorphonuclear and accumulation azithromycin of REFERENCES 2 Hacettepe University, Faculty ofPharmacy, DepartmentofAnalytical Chemistry, 06100Sıhhiye,Ankara, Türkiye PREPARATIONS AND STRESS TESTING FOR DETERMINATION OF OF DETERMINATION FOR TESTING STRESS AND PREPARATIONS OF AZITHROMYCIN AND ITS IMPURITIES IN PHARMACEUTICAL PHARMACEUTICAL IN IMPURITIES ITS AND AZITHROMYCIN OF to the 50 S ribosomal subunits of susceptible bac otic with a 15-membered azalactone ring. It binds antibi- macrolide semisynthetic a is zithromycin International Symposium onDrugResearch &Development 2011 1 Deva HoldingA.Ş.34303,Küçükçekmece -İstanbul, Türkiye DEGRADATION PRODUCTS DEGRADATION Şeyda İLTER * [email protected] DRD 2011 P-065 120 - - 1 , and reduction wereand reduction determined by validated UPLC method. oxidation hydrolysis, base hydrolysis, acid photolysis, ture, tempera- with occurred products degradation the and tions time and low analysis cost was compared with HPLC method. retention short resolution, high with method UPLC rugged (240nm). and UVdetector (65 : 35, v/v) pH = 6.0 mobile phase with 0.4 mL/min flow rate acetonitrile / buffer phospate mM 5 using performed were impurities its and Azithromycinsize. of UPLC anaysiscal The with Acquity BEH C18, 50 x 2.1 mm column with 1.7 µm - parti for the analysis of Azithromycin and its impurities were done conditions the of Optimization method. chromatographic developed the by analysed conditions stress the to drug of exposure the by formed products degradation of amounts The preparation. pharmaceutical the to applied and dated vali- fully was method UPLC.This using accuracy good with azithromycinof determination the enables which approach, cording to theICHguidelines4. ac method the of validation the and preparation ceutical - pharma the from UPLC by impurities its and Azithromycin determine to is study this of aim The back-pressures3. tem 4. 3.

Sedef KIR nentoa Cneecs n amnzto, Guidance Harmonization, on Conferences International of Advantages P. Solich L, Matysova L, Novakova hraetcl rprtos xoe t srs condi- stress to exposed preparations Pharmaceutical and rubbest sensitive, accurate, precise, selective, The sensitive highly and selective fast, a describes study This n muiis n e Du Pout. 3() Federal Q3B(R). Register. 65: 44791-44797,2000. Products. Drug New in Impurities on 68: 908-918,2006. Talanta analysis. pharmaceutical in UPLC of application Biology 385:1179-1192,2009. 2,* - POSTER PRESENTATIONS - 2 , Zeki TOPÇU 2 Acknowledgement: This study is supported by grants tions of pathological consequence using a derivative of the method, termed as reverse hybrid. Our laboratory employs yeast hybrid technology in a number of research with phar maceutical implications. We are currently verifiying a number of interactions that pulled we up on cDNA library screen for selected bait constractions. Our results are discussed in terms of implications and limitations of this technology in drug screening. TBAG108T945. TUBITAK, from - - 121 P-066 DRD 2011 DRD Pakize CANTÜRK , Pakize 1 Sevil ZENCİR Sevil International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Department of Biochemistry, Faculty of Science, Ege University, 35100 İzmir, Türkiye 35100 İzmir, Ege University, of Science, Faculty Department of Biochemistry, 1

IN DRUG SCREENING; ITS IMPLICATIONS AND LIMITATIONS east hybrid is a powerful technique in - determin ing of molecular Variations this interactions. - tech and yeast-1-hybrid hybrid, yeast-2- as such nology Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Ege University, 35100 İzmir, Türkiye 35100 İzmir, Ege University, of Pharmacy, Faculty Biotechnology, Department of Pharmaceutical 2 Y WHAT CAN YEASTWHAT HYBRID TECHNOLOGY TELL US IN DRUG SENSITIVITY tions, tions, respectively. Considering the fact that most pathological of outcomes in mammalian the cells arise as a result of inappropriate molecular interactions, determination of drug contemprorary in step essential an is interactions these The design. synthetic compounds of pharmaceutical - signifi cance can be tested for their ability to interfere the interac yeast-3-hybrid yeast-3-hybrid provides us an extended tool in identifying protein-protein, DNA-protein and receptor-ligand interac POSTER PRESENTATIONS ae. cmo apoc fr h pK the for approach common A water. clude glipizide, gliclazide, [1]. glibenclamideandglimepride in- which sulfonylureas generation second the and formin met are diabetes 2 Typefor medications prescribed monly that help reduce blood sugar levels. Currently the most com- administeredhypoglycemicorally with agents possible now tion. Treatment of type-2 diabetes (non-insulin dependent) is 2. h dsoito cntn o 4sbtte ezn sulfon- benzene 4-substitue of constant dissociation the study, this In recommended. are co-solvent of percentages ganic mixtures. Typically, at least three and up to six different compoundsinsoluble aqueous involves hydro-or of use the 1. Barbosa J, Barron D, Buti S. Chromatographic behaviour Chromatographic S. Buti D, Barron J, Barbosa Sweetman SC (2009) Ed., Martindale, The Extra Pharma- Extra The Martindale, Ed., (2009) SC Sweetman Glibenclamide and gliclazide are practically insoluble in insoluble practically are gliclazide and Glibenclamide of ionizable compounds in Liquid Chromatography.Liquid Part in compounds ionizable of copoeia, 36 REFERENCES T DETERMINATION OF DISSOCIATION CONSTANTS OF GLICLAZIDE GLICLAZIDE CONSTANTSOF DISSOCIATION OF DETERMINATION 3 1 Ankara University, Faculty ofPharmacy, DepartmentofAnalytical Chemistry, 06100Ankara, Türkiye of insulin, a hormone that regulatesabsorp that sugar hormone a insulin, of where in the body becomes resistant to the effects disorder metabolic long-term a is diabetes ype-2 Bitlis Eren University ,Science &Literature Faculty, DepartmentofChemistry,13000 Bitlis,Türkiye AND GLIBENCLAMIDE WITH POTENTIOMETRİC METHOD IN IN METHOD POTENTIOMETRİC WITH GLIBENCLAMIDE AND th 2 Ed., Pharmaceutical Press, London. Hitit University, Science &Literature Faculty, DepartmentofChemistry, Çorum,Türkiye

TETRAHYDROFURAN-WATER BINARY MIXTURES BINARY TETRAHYDROFURAN-WATER International Symposium onDrugResearch &Development 2011 Dilara BAŞAT Figure 1.Structureofgliclazideandglibenclamide. a esrmns of measurements 1, * * [email protected] , NurullahŞANLI DRD 2011 P-067 122 - - - relationships (LSER) method was used to correlate pK energy solvation linear the and examined were properties the SPARC on-linepK by predicted values the with compared been have medium calculation of the pK allowed obtained equations [2].The (β) basicity accepting bond- hydrogen- solvent and (a) acidity –donating bond drofuran–water mixture. The pK 3. with solvent dipolarity/polarizability (п dipolarity/polarizability solvent with potentiometrically. at five different percentages (40, 45, 50, 55, and 60% (v/v)) by mixtures tetrahydrofuran–waterbinary in determined been (Figureglibenclamide and havegliclazide 1) groupof amide PR O-ie acltr Uiest o Goga USA, Georgia, of University Calculator, On-line SPARC http://ibmlc2.chem.uga.edu/sparc/index.cfm tetrahydrofuran-water. Anal 389:31-42,1999. ChimActa in buffers standard for values pHs and pKa scale, pH 1. The relationships between pK between relationships The 2 , SibelA.ÖZKAN a values of the substances in any tetrahy a calculator [3]. 3 a values obtained in aqueous a values and different bulk different and values * ), solvent hydrogen- solvent ), a values - POSTER PRESENTATIONS - of a - val a ,a, β) * values a calculator, a 2 values have been calculated from a values with solvent properties (п a Güleren ALSANCAK ALSANCAK , Güleren 2 values determined in tetrahydrofuran–water a The major drawback in the determination of pK of determination the in drawback major The Drugs Today 40(7): 633, 2004. Today Drugs North 26: 553, 1997. Am constants and preferential solvation in tetrahydrofuran- 18: 3281-3288, 1999. Polyhedron mixtures. water In the study tetrahydrofuran–water binary mixture R.R. Henry, Thiazolidinediones. Endocrinol Metab Clin Baron D, Buti S, Ruiz M, Barbosa J. Evaluation of acidity 3. 4. mixtures. mixtures. These values have been compared with the values predicted by the SPARC on-line pK and relative and permittivityrelative examined were and the linear used was method (LSER) relationships energy solvation to correlate pK ues of these drugs are their very low aqueous solubility because of their Very hyrophobic nature. often, the main difficiulty in the determination of aqueous pK drug candidates is their aqueous insolubility that forc solvent. es the use of a hydroorganic dissocia- the and solvent hydroorganic as selected was tion constants of rosiglitazone and pioglitazone have been determined in these mixtures (40- 60% (v/v)) in accordance with IUPAC procedures by - potentiometri cally. Potentiometry has been the most useful - tech niques for the determination of equilibrium constants and accuracy their of because mixture, hydroorganic in reproducibility. The relationships between pK ACD Lab, Marvin Lab, Sketch. ACD [4]. The The aqueous [4]. pK the pK - - 123 P-068 DRD 2011 DRD [email protected] * BINARY MIXTURES Many Many patients

, Ebru ÇUBUK DEMİRALAY 1,* International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Dilara BAŞAT Dilara values of rosiglitazone and pioglitazone (ACD a

uman diabetes is currently classified into two two into classified currently is diabetes uman general categories: Type I, or insulin-dependent diabetes mellitus, and Type II, or non- Bitlis Eren University, Science & Literature Faculty, Department of Chemistry, 13000 Bitlis, Türkiye 13000 Department of Chemistry, Faculty, & Literature Science University, Bitlis Eren pK 1

Süleyman Demirel University, Science & Literature Faculty, Department of Chemistry, 32260 Isparta, Türkiye 32260 Isparta, of Chemistry, Department Faculty, & Literature Science University, Demirel Süleyman 2 PIOGLITAZONE AND ROSIGLITAZONE IN TETRAHYDROFURAN-WATER REFERENCES ride: A new formulation therapy for type 2 diabetes. the pathogenesis and treatment of noninsulin-dependent diabetes mellitus. Am J Med 74 (Suppl 1A): 52-81, 1983. Cox, Cox, S.L. Rosiglitazone maleate/metformin hydrochlo DeFronzo DeFronzo RA, Ferrannini E, Koivisto V. New concepts in H POTENTIOMETRIC DETERMINATION OF DISSOCIATION FORCONSTANTS Lab). 2. 1. Figure Figure 1. insulin-dependent diabetes 1. mellitus with type II diabetes require treatment with with type than more treatment II diabetes require one antihyperglycaemic drugs to achieve optimal gly caemic control. The thiazolidinediones are novel oral - con glycaemic improve that drugs antihyperglycaemic trol primarily by decreasing insulin by resistance sensi- tizing the skeletal muscle, liver and adipose tissue to the actions of 2. insulin Rosiglitazone and pioglitazone are in a class of drugs called thiazolidinediones. Rosi- glitazone contains a thiazolidinedione core, but differs from pioglitazone in the presence of an aminopyridyl 1). side chain3 (Figure POSTER PRESENTATIONS netic parameters (t parameters netic - pharmacoki some trimatezidine, of pharmacokinetics the on food of influence the investigate Todays. 10 of washout periods by separated were Treatments products. zidine - trimeta branded different two given been have who teers 1. A Guidance for Industry. Food-Effect Bioavailability and Fed Bioequivalence Studies. FDA, CDER,December 2002. REFERENCES EFFECT OF FOOD ON THE PHARMACOKINETICS OF TRIMETAZIDINE TRIMETAZIDINE OF PHARMACOKINETICS THE ON FOOD OF EFFECT Emel D.KURTOĞLU atn ad e cniin i 3 haty volun- healthy 36 in conditions fed and fasting in conducted been has study bioequivalence crossover period, four open-label, randomised, max , C , max International Symposium onDrugResearch &Development 2011 and AUC and 1 Novagenix Bioanalytical DrugR&DCentre, Ankara, Türkiye 1,* 2 Gazi University, Faculty ofPharmacy, Ankara, Türkiye , Onursal SAĞLAM 0-tlast ) were evaluated as evaluated were ) * [email protected] DRD 2011 P-069 124 1 , SamiEREN 2. dine isnoteffected by food. reference products. and test both in evaluated, were conditions fed and fasting in trimetazidine of parameters pharmacokinetic between difference of intervals confidence 90% Thedesign. paralel a

W/W/419 Rv1 Dat Lno, MA July EMEA, 2008. London, Draft, Rev.1, QWP/EWP/1401/98 Bioequivalence.CPMP/ of Investigation the on Guideline - trimetazi of bioavailability the that showed results Our 1 , ErkinALKAN 1 , Tuncel ÖZDEN 2 POSTER PRESENTATIONS - - - Samsun 1 , A. Nur ONAR 2 tion method for 3-nitrotyrosine [Dissertation], (Türkiye), Ondokuz Mayıs University Institute of Natural 2008. Sciences, In this work we tried to improve this strong method. It tively. There is There a peak at the tively. reduction potential of 3-nitroty rosine arising from both synthetic and natural cerebrospinal fluid. This peak moved to more negative potentials while pH of supporting electrolyte was increased and emerged at more positive potentials when pH was decreased in parallel to 3-nitrotyrosine peak. This behaviour leads to higher LOD and values. Comparison LOQ of calibration curves were per of absence and presence the in prepared were those formed, to pH 9.0 fluid and at pH 7.2 in order cerebrospinal synthetic fluids. cerebrospinal in real 3-nitrotyrosine quantify is preferred to prepare the calibration curve in the presence of synthetic cerebrospinal fluid as recommended analysis of biological in fluids. The irreversible reduction the peak of 3-NT was observed at -774 mV and -750 mV (vs. Ag/AgCl, 3M KCl) in phosphate buffers at pH 9.0 and pH 7.2 respec - - 125 M) P-070 -10 DRD 2011 DRD Ebru TÜRKÖZ ACAR , Ebru TÜRKÖZ [email protected] * 1,* 3-NITROTYROSINE J Clin Invest 109: 1287- International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Muharrem ÖZTÜRK Muharrem

M) values. The method was applied 3-nitro

-9 Faculty of Pharmacy, Yeditepe University, 26 Ağustos Campus, 34755 Ataşehir, İstanbul, Türkiye İstanbul, Campus, 34755 Ataşehir, 26 Ağustos University, Yeditepe of Pharmacy, Faculty 2 yrosine residues in proteins including enzymes are enzymesare including proteins in residues yrosine chemically converted to 3-nitrotyrosine by per oxynitrite. 3-Nitrotyrosine is currently being used AN ELECTROCHEMICALLY ACTIVE OXIDATIVE STRESS MARKER: Department of Chemistry, Art and Sciences Faculty, Ondokuz Mayıs University, 55139 Samsun, Türkiye 55139 Ondokuz Mayıs University, Faculty, Sciences Art and Department of Chemistry, 1 T 1289, 2002. REFERENCES - determi voltammetric wave square stripping Adsorptive Türköz Türköz Acar E. Development of quantitative - determina Hurst SK. Whence nitrotyrosine? 2. 1. and LOQ (»10 tyrosine determination in cerebrospinal tyrosine fluid determination in after- cerebrospinal precipita tion of proteins. However the analysis of cerebrospinal fluid for nitrotyrosine gave false positive results, possibly due to 2. reactions of proteins the precipitation nation nation of 3-nitrotyrosine was developed by Acar and Onar (»10 LOD low very a with 9 pH at buffer phosphate using as a marker for oxidative stress damage1. stress oxidative as a marker for POSTER PRESENTATIONS HRMS data. 2. 1. tures of the compounds were confirmed by UV, IR, UV,by confirmed were compounds the of tures struc The method. dilution micro the by activities tifungal an- and antibacterial vitro in for evaluated and synthesized were analogues benzimidazole novel six their and azoles SYNTHESIS AND A AND SYNTHESIS 1 2 Department ofPharmaceutical Microbiology, Faculty ofPharmacy, EgeUniversity, 35100Bornova, Izmir, Türkiye Navarrete-VaÂzquez G, Cedillo R, HernaÂndez-Campos HernaÂndez-Campos R, Cedillo G, Navarrete-VaÂzquez M. İşcan B, Can-Eke ED, Özdamar C, Kuş G, Ayhan-Kılcgil iaaii atvt o 2-(trifuoromethyl)-benzimidazole of activity tiparasitic an- and Synthesis R. Castillo M, HernaÂndez R, CorteÂs R, Morales J, Valdez F, HernaÂndez-Luis, L, YeÂpez A, 1, 2007. imidazole derivatives. Arch Pharm Chem Life 34: 607– Sci benz- new some of capacities antioxidant and Synthesis REFERENCES n hs td, he 2-substitutedphenyl-1H-benzimid- three study, this In 1 Department ofPharmaceutical Chemistry, Faculty ofPharmacy, EgeUniversity, 35100Bornova, İzmir, Türkiye antiparasitic, antiproliferative,1-4. antiviral activities antioxidan, as such effects biological of types ous vari- with associated been have H-Benzimidazoles Görkem SARIKAYA International Symposium onDrugResearch &Development 2011 ntimicrobial 1, * , A.Selcen ALPAN * [email protected] D 1 H NMR, H erivatives DRD 2011 P-071 Activity 126 - pound, Ceftazidime. com- standart the to compared results similar or equal sess pos- ring 1H-benzimidazole on substituent hydroxyphenyl bearing intermediates 2-(1H-benzimidazole-2-yl)phenyl tive to gram (+) bacteria than gram (-) bacteria. Furthermore, 90028. on activitiy antifungal significantany cansATCC 90028. Thesynthesizedshow not compounds did against activity ATCCantifungal for and 29213 Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus of strains ATCC against tivity 4. 3. 1 , Hüseyin TAŞLI [4] M. Castelli, T, Rossi, M., Malagoli, M., Roberti, L., Garuti, l o te opud wr tse fr niatra ac antibacterial for tested were compounds the of All 10: 2193-5,2000. Lett Chem Med Bioorg derivatives. benzimidazole-4,7-dione some of activity antiproliferative and Synthesis derivatives. Bioorg ChemLett Med 11:187-90,2001. 3(3): 305–9,2009. China Eng Chem Frontderivatives. azole-4-carboxamide synthesis,H-benzimid- and antiviralof 2-aryl-1 properties Luo X, Zhang Z, Yang Y, Xue F, Xiu N, She Y. Design, Y.She N, Xiu F, Xue Y,Yang Z, Zhang X, Luo It is found that all of the compounds are more effec more are compounds the of all that found is It

of N ew 2 , H.SemihGÜNEŞ 1 H -B shrci coli Escherichia enzimidazole ATCCalbicansCandida 1 Candida albi - Candida TC 25922, ATCC o-

- - POSTER PRESENTATIONS ------Pseudomo RSSK RSSK 95047 . . A range wide 3 produced 14mm, , antimicrobial and , antimicrobial has been reported reported been has 3 1 1 4,5 O 0157:H7 RSSK 234 and H O O 1 ) are in progress. in are ) 3 H - O J Antibiot 61(4): 245-249, 2008. 245-249, 61(4): Antibiot J 2 have demonstrated the medicinal medicinal the demonstrated have Staphylococcus aureus Staphylococcus Erdal BEDİR , Erdal 6,7 6,7 2 g g per disc in disc diffusion The assay. Escherichia Escherichia coli m , , Aspergillus flavus. Aspergillus - anti and cyclearrest Cell H. Osada T, Mayumi T, Nishikiori Lett Cancer derivatives. its and pironetin of activity tumor 126: 29-32, 1998. Gibepyrones: a -pyrones from Reyes JF. Rojas F, Quílez JF, 49: 141-150, 1993. Tetrahedron fujikuroi. Gibberella ity of 6-pentyl-2H-pyran-2-one and its analogs. J Agric Chem 45: 2774-2776, 1997. Food from isolated derivatives a 2-pyrone fun marine-derived gus Kondoh M, Usui T, Kobayashi S, Tsuchiya K, Nishikawa K, Oltra JE, Barrero AF, Herrador MM, Cabrera E, Sanchez JF, SR, HG, Parker Culter Jacyno JM, Hillf RA. Biological activ Lin A, Lu X, Fang Y, Zhu T, Gu Q, Zhu W. Two New 5-hydroxy- New Two W. Zhu Q, Gu T, Zhu Y, Fang X, Lu A, Lin

methicillin-resistant methicillin-resistant (MRSA) at 700 and elucidation structure studies bioactivity for the re ( compounds maining of bioactivities such as, antitumour as, such of bioactivities activities antifungal is no its there for an data agent, as a cytotoxic recently 11mm and 10 mm zones inhibition against bacteria, bacteria, fungus, plant, insect and animal and systems, processes biological of types different many in part take biosyn key as organisms, other against defense as such and as metabolites intermediates, thetic Although 2-pyrones. of importance timicrobial activity [8]. Compound nas aeruginosa 5. 6. 7. 8. Funda N. YALÇIN , Funda 1 ------127 ) ) by P-072 DRD 2011 DRD 1 strain [email protected] * Aspergillus Flavus Türkiye İzmir, 35100 Bornova, Ataç UZEL , Ataç ) from fermenta from ) 1, * 3 - sp. sp. NF 00659. I. Tax 1 -pyran-2-one -pyran-2-one ( Marine Mycology: The H Aspergillus flavus Aspergillus Aspergillus International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International is is a cyclic six-membered unsatu Ş.Orçun KALKAN Ş.Orçun

ew antimicrobial molecules have attracted great resistance antibiotic of emergence to due interest sourc terrestrial the Since bacteria. pathogenic in Hacettepe University, Faculty of Pharmacy, Department of Pharmacognosy, 06100 Ankara, Türkiye 06100 Ankara, Department of Pharmacognosy, of Pharmacy, Faculty University, Hacettepe 2 Ege University, Faculty of Science, Department of Biology, Basic and Industrial Microbiology Section, Microbiology Basic and Industrial Biology, Department of of Science, Faculty Ege University, Ege University, Faculty of Engineering, Department of Bioengineering, 35100 Bornova, İzmir, Türkiye İzmir, Bornova, of Bioengineering, 35100 of Engineering, Department Faculty Ege University, 1 3

ANTIMICROBIAL METABOLITES FROM A MARINE DERIVED FUNGUS In In our we study, isolated 42 fungal strains from dif shikiori T. NF00659A1, A2, A3, B1 and B2, novel antitumor antitumor novel B2, and B1 A3, A2, NF00659A1, T. shikiori antibiotics produced by drug discovery: current status and future potential, in 2000, 6. the Sea Basel, Drugs from , Karger Publishers: and mimetics: isolation, characterization and biological Rep 22: 369-385, 2005. Prod Nat activity. REFERENCES 1979. York, New Press: , Academic Higher Fungi onomy, fermentation, isolation and biological activities. J activities. biological and isolation fermentation, onomy, 50: 314-317, 1997. Antibiot J. J. Kohlmeyer and E. Kohlmeyer, Ni - S, H, NishikioriFujita SuzukiT, K,Yoshida Kuwahara A, P. R. P. Jensen and W. Fenical, Marine microorganisms and McGlacken GP, Fairlamb IJS. 2-Pyrone natural products N using using NMR. 2-Pyrone ferent ferent sponge and marine screened their activity against a sediment panel of antibiotic re samples and An sistant test microorganisms. showed potent activity against test microorganisms, and bioactivity guided isolation studies were ( carried isolated were molecules Three out. and one of of the was broth them tion identified strain, as 4-(hydroxymethyl)-5-hydroxy-2 2. 4. 1. 3. rated rated ester, and its derivatives are highly abundant in es were extremely exploited for natural antibiotic producer microorganisms, studies were shifted to 1. recently marine The sources marine microorganisms can produce quite potent metabolites different than the terrestrials because of the different conditions in marine environments such as 2. compositions and nutrient temperature salinity, pressure, POSTER PRESENTATIONS albumin nanoparticles in order to obtain targeted drug de drug targeted obtain to order in nanoparticles albumin magnetic loaded doxorubicin synthesized we aim, this For stopped with a powerful magnetic ﬁeld in the target area [3]. then and stream, patient’sblood a into injected compound, magnetic a to bound is radioisotope therapeutic or drug a targeting, magnetic In site. disease localized a to drug a ing deliver of method efﬁcient very a is carriers particulate by delivery drug Magnetic [2]. delivery candidatefordrug ideal an it make immunogenicity and toxicity of lack and ability biodegrad- availability, ready tumor, in uptake preferential its as well as properties These setting. clinical drug the in a carrier as role increasing an playing is Albumin [1]. heart the in concentrations drug reduced in resulting drug, the of riers,pharmacodistribution the in change a which engender car drug use to is doxorubicin-relatedtoxicity ameliorating to approach different A death. and failure heart congestive to lead may cardiomyopathy,which is drug this for toxicity 2. 1. D NANOSPHERES WITH A SIMPLE METHOD AND IN VITRO DOXORUBICIN DOXORUBICIN VITRO IN AND METHOD SIMPLE A WITH NANOSPHERES rt F Abmn s du crir Dsg o prodrugs, of Design carrier: drug a as Albumin F. Kratz Waterhouse DN, Tardi PG, Mayer LD, Bally MB. A compari- Release 132:171-183,2008. Release drug conjugates and nanoparticles. Journal of Controlled 2001. 903-920, (12): 24 Safety Drug form. free in administered drug with doxorubicin of formulations liposomal of son REFERENCES SYNTHESIS OF DOXORUBICIN INCORPORATED MAGNETIC ALBUMIN ALBUMIN MAGNETIC INCORPORATED DOXORUBICIN OF SYNTHESIS group of anticancer agent. The therapy-limiting The antibioticagent. anticancer of group anthracycline the of member used widely most and known best the is oxorubicin Ege University, Faculty ofScience, Biochemistry Department,35100İzmir, Türkiye International Symposium onDrugResearch &Development 2011 Güliz AK * RELEASE STUDIES RELEASE , HabibeYILMAZ,ŞenayŞANLIER *[email protected] DRD 2011 P-073 128 - - - 5. 4. 3. tive release. Then, obtained results were compared according to cumula- spectrophotometrically. analyzed was amount doxorubicin and taken were samples intervals predetermined At 7,4. 6, 5, pH at studies release vitro in for used were doxorubicin free and nanoparticles albumin magnetic incorporated cin Doxorubi- capacity. loading drug and effiency desolvation nanoparticles, of size on based determined were conditions optimum and researched were amount glutaraldehyde and albumin, doxorubicin and magnetic agent concentration, pH of effect The purified. and centrifuged was solution sulting re h, 24 of end the Atcrosslinking. particle induce to added was glutaraldehyde process desolvation After temperature. room at rpm) (480 stirring continious under system pump a by rate flow of ml/min desolvating 4 with then added was water, ethanol agent, distilled ml 1 in dissolved were described [5]. 25 mg albumin, 1 mg doxorubicin and Fe and doxorubicin mg 1 albumin, mg 25 [5]. described previously as method co-precipitation by synthesized was eye rslnig ih mnr oiiain 4. Fe [4]. modification minor a with crosslinking dehyde glutaral - by followed technique desolvation a by prepared were nanoparticles Albumin release. controlled and livery The study of novel Fe3O4@γ--Fe2O3 core/shell nanoma- Fe3O4@γ--Fe2O3core/shell novel of study The H, Briesen von N, VogelV,Dinauer S, Balthasar K, Langer systems. therapeutic modulated Magnetically UO. Hafeli and MagneticMaterials321: 1052-1057,2009. Magnetism of Journal properties. improved with terials ofPharmaceuticsJournal 257:169-180,2003. human serum albumin (HSA) nanoparticles. International for process preparation the of Optimization D. Schubert ofPharmaceuticsInternational Journal 277:19-24,2004. 3 3 O O - 4 4

POSTER PRESENTATIONS - - - - Mean recover - Vali used. softwarewas 32 vision with loaded computer a to dation parameters such as limit of detection (LOD), limit of quantification (LOQ), linearity, precision, accuracy, recovery, Confer International the in reported as studied are specificity ence on Harmonization Guidelines. Standard stock solution of etodolac (100 μg/mL) was prepared in methanol. Spec trophotometrically, etodolac were determined by means of UV absorbance values (A) at 272 nm. Linearity range Beer’s law was found as 3-20.0 μg/mL. The calibration curve have linearity with correlation coefficient r=0.999. ies and the relative standard deviations of the method were method Developed respectively. 2.51%, and % 98.21 as fond was successfully applied to etodolac in pharmaceutical for mulations. - - 129 P-074 DRD 2011 DRD Yücel KADIOĞLU , Yücel TURAN Atakan Alptuğ ATİLA, International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International ETODOLAC IN PHARMACEUTICAL FORMULATIONS

- non-steroi used are animals domestic and umans their to due (NSAIDs) drugs anti-inflammatory dal anti-inflammatory, analgesic and anti-pyretic - ef SPECTROPHOTOMETRIC METHOD FOR THE DETERMINATION OF Department of Analytical Chemistry, Faculty of Pharmacy, Atatürk University, 25240, Erzurum, Türkiye 25240, University, Atatürk of Pharmacy, Faculty Chemistry, Department of Analytical

Etodolac Etodolac was kindly supplied from Novagenix - Pharma H ceutical ceutical Industry (Ankara, Turkey). Acetaminophen as inter fects1. Etodolac b]- (1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4- NSAID, well-tolerated and effective an is acid) indole-1-acetic and is indicated for the treatment of analgesia and for the osteoarthriarthritis- and rheumatoid of symptoms and signs tis2. nal standard (IS) was obtained from Sigma-Aldrich (product spectropho UV-Vis beam double Thermospectronic USA). of tometer (HEλIOSβ) with a fixed slid width (2 nm) connected POSTER PRESENTATIONS Fe in shown was tin - cispla of structure The 2. expected been have effects tumor tumor is very short, no significantly high and prolonged anti- retentionof the in period time circulatingthe blood and the into passed rapidly is cisplatin weight, molecular low its of because thus nephrotoxicity acute and disturbance, testinal neurotoxicity,as gastroinsuch - effects side severe its to due limited is use clinical its However, etc. cancer lung and ian ovar treat to used widely that agent anticancer an is inum) tively low1. Cisplatin antigenicity (cis-dichlorodiamminoplat not usually contaminated with pyrogens and possesses rela- is sterilized, be can inexpensive, is it Moreover, crosslink. to carrying: for example, it is biodegradable, non-toxic and easy the other synthetic polymers, which make it suitable for drug- 3. 2. 1. eai nnprils Gltn aoatce wr synthe were nanoparticles Gelatin nanoparticles. gelatin magnetic loaded cisplatin prepare to chosen was B type tin I area3. targeted the in drug of localization PREPARATIONAND 3 G O Mederios SF, Santos AM, Fessi H, Ellaissari A. Stimuli-re A. Ellaissari H, Fessi AM, Santos SF, Mederios Ding D, Zhu Z, Liu Q, Wang J, Hu Y, Jiang X, Liu B. Cisplatin- Gaihre B, Aryal S, Khil MS, Kim HY. Encapsulation of Fe3O4 sponsive magnetic particles for biomedical applications. biomedical for particles magnetic sponsive 10857,2011. tics EJPB Biopharmaceu- and Pharmaceutics of Journal European tumors. in penetration and vivo in efficiency antitumor loaded gelatin-poly(acrylic acid) nanoparticles: Synthesis, Microencapsulation 25(1):21-30,2008. of Journal dispersion. colloidal the of stability and size in gelatin Effect nanoparticles: of different paramaters on REFERENCES 4 can be coated with polymers and allows to control the has a number of advantages in comparison with comparison in advantages of number a has It applications. biomedical and biotechnological elatin, a natural macromolecule, is widely used in . Magnetic nanoparticles such as such nanoparticles Magnetic 1. Figure Ege University, Faculty ofScience, Biochemistry Department,35100İzmir, Türkiye International Symposium onDrugResearch &Development 2011 MAGNETIC GELATIN NANOPARTICLES GELATIN MAGNETIC IN VITRO IN Habibe YILMAZ n this study,gela- this n *[email protected] RELEASE STUDIES OF CISPLATIN LOADED LOADED CISPLATIN OF STUDIES RELEASE * , GülizAK,ŞenayŞANLIER DRD 2011 P-075 130 - - - - 5. 4. . Synthesis of magnetic agent, Fe agent, magnetic of Synthesis 4. nanoparticles tin pure water and 2 ml aceton added dropwise to prepare gela- discarded. the second step,In precipitate redissolved in 1 ml gelatin weight molecular high and aceton ml 1 with tated precipi- solution gelatin 5% step, first the In studies. earliest the in described as method desolvation two-step by sized Te fet f h matrix Feconcentration, the of effect The 5. nanoparticles gelatin magnetic form to used and method co-precipitation by performed carried out. carried were studies nanoparticles gelatin magnetic from release cisplatin vitro in Moreover, determined. acetone agent, ing desolvat of ratio flow concentration, glutaraldehyde agent Gao Q, Chen F, Zhang J, Hong G, Ni J, WeiX, Ni F,WangD. G, Q,Chen Hong Gao J,The Zhang ZwiorekBourquin BattianyC, K., J, WinterEndresG, En- S, Magnetic Materials321:1052-1057, 2008. and Magnetizm of Journal properties. improved with als nanomateri- core/shell Fe3O4@g-Fe2O3 novel of study Research 25(3):551-562,2008. Pharmaceutical oligonucleotides. CpG of effects latory immunostimu- the increases strongly nanoparticles tin gela- cationic by Delivery C. Coester G, Hartmann S, dres JourofPharmaceuticsInt 403:139-161,2011. Figure 1. The ofcisplatin. structure 3 O 4 (magnetite) amount, pH, cross-linking cross-linking pH, amount, (magnetite) 3 O 4 , was , - POSTER PRESENTATIONS - - - Vitis Vitis vinifera leaves. Phy 2 , A. Nur ONAR 1,* - natural a is trihydroxy-trans-stilbene) 5 4´, (3, Resveratrol It is aimed to show the presence of Cu (I) in the Cu (II) - Pharmacol 55: 1399-1404, 1998. 55: 1399-1404, 1998. Pharmacol Zhang HY, Priyadarsini KI. Evaluation of new copper(II) curcumin complex as superoxide dismutase mimic and 811-822, 39: Med Biol Radic Free reactions. radical free its 2005. and cataltic actvity of metal-phenolic complexes. J Phys Chem B 109: 24197-24202, 2005. ostilbene as a phytoalexin from tochemistry 18: 1025-1027, 1979. Barik A, Mishra B, Shen L, Mohan H, Kadam RM, Dutta S, M. Radical scavenging Tulsi Harbir SM, Sudhir K, KS, Ashis Cornford CA, Langcake Pryce P, RJ. Identification of pter phoretic phoretic experimental conditions were selected as: +23kV applied potential, 20°C temperature while using fused silica length. and 50cm with 50μm inner diameter column . This This 6. metabolite secondary plant a phytoalexin, occurring ly polyphenol is supposed to be responsible for beneficiary wine. health effects of red complex by capillary resveratrol Borate buf- electrophoresis. fer (0.05M), was chosen as running electrolyte. Copper (II) and copper (I) - resveratrol complexes were prepared with electro Capillary pHs. various at ratios ligand-metal different 4. 5. 6. ------131 P-076 DRD 2011 DRD [email protected] . * 4 Enhanced Enhanced ELECTROPHORESIS . On the other hand hand other the On . Samsun, Türkiye 55600 Terme, University, 1,2,3 Behice YAVUZ ERDOĞAN YAVUZ Behice International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

STUDY OF RESVERATROL-COPPER COMPLEXES BY CAPILLARY Department of Chemistry, Art and Sciences Faculty, Ondokuz Mayıs University, 55139 Samsun, Türkiye 55139 Ondokuz Mayıs University, Faculty, Sciences Art and Department of Chemistry,

2 n biological systems redox active free metals (e.g. copper, copper, (e.g. metals free active redox systems biological n reac producing radical free catalyze manganese) and iron absence their in slow are that tions There There exists the possibility of reduction of metal ions by Guo Q, Zahao B, Li M, Shen S,Xin W. Studies on protective protective on Studies W. S,Xin Shen M, Li B, Zahao Q, Guo mechanism of four components of green tea polyphe Spitz DR. LW, Y,Oberlet HL,Ridnour LA,Tao REFERENCES Biochim synaptosomes. in peroxidation lipid againts nols Acta 1304: 210-222, 1996. Biophys gamma-glutamyl transpeptidase expression and selec tive loss of CuZn superoxide dismutase in hepatic iron Radic Biol Med 24: 545-555, 1998. Free overload. noxyl radical intermediates in lipid antioxidant action of Biochem culture. hepatocyte rat iron-treated in myricetin Brown KE, Kinter MT, Oberley TD, Freeman ML, Frierson phe of Involvement J. Cillard O, Sergent V, Abelea I, Morel

Department of Food Technology Programmes, Technical Vocational School of Higher Education, Ondokuz Mayıs School of Higher Education, Vocational Technical Programmes, Technology Department of Food I 1 phenols. The The phenols. presence of a different oxidation state of Cu in impor have may ligand antioxidant phenolic a with complex tant tant implications in the biological reactions and therefore be studied in detail5. has to several copper, iron and manganese complexes have been re been have complexes manganese and iron copper, several su of dismutation the catalyzing of ability the exhibit to ported reduced the of presence the that claimed is It radicals. peroxide be respon may of complexes in solutions ions of metal forms activity like (SOD) dismutase superoxide this for sible 1. 2. 3. POSTER PRESENTATIONS Robinson buffer solutions prepared in 20% and 30% aceto 30% and 20% in prepared solutions buffer Robinson Britton- in voltammetry pulse differential by investigated was films (NIP) non-imprinted and imprinted on doxycyline of behavior voltammetric The electrode. graphite onto pencil a pyrrole of electropolymerization the during cyline) (doxy molecule template a of incorporation by prepared was (OPPy) investigated.overoxidizedpolypyrrolewere The doxycyline for properties recognition its and film (MIP) mer treatment andsensitivity. pre- sample like advantages well-known the to due used also is detection Electrochemical used4. been have drugs determination of tetracyclines in pure form and in veterinary the for methods Several humans3. in resistance bacterial to lead can antibiotic, of doses level low containing foodstuffs and environment samples2. Even more important, consumed products biological in antibiotics of residues the over raised are concerns health, public on effects adverse their of cause be time, same the At additives1. feed as well as medicines 2. 1.

amperometric of EvaluationD.E. Moore A.G., Kazemifard In In this work, preparation of a molecularly imprinted poly tion of tetracyclines. J Chromatogr A 1118: 35-40,amperometric 2006. multicycle step waveform forthe determina Cai Y, Cai Y, Shi Y, Mou S, maceutical andBiomedicalAnalysis 16:689-696,1997. Lu Y. Optimizing Phar of the Journal integrated formulations. pharmaceutical in pulsed nants contami- common their and antibiotics tetracycline of determination liquid-chromatographic the for detection REFERENCES T ria, being widely used in human and veterinary veterinary and human in used widely being ria, bacte Gram-negative and Gram-positive of range he tetracycline antibiotics are active against a wide Süleyman Demirel University, Faculty ofScience andArt,Dept.ofChemistry, Isparta, Türkiye ELECTROCHEMICAL DETERMINATION OF DOXYCYCLINE OF DETERMINATION ELECTROCHEMICAL Berrin GÜRLER International Symposium onDrugResearch &Development 2011 * , Sabriye PERÇİNÖZKORUCUKLU, EsengülKIR * [email protected] DRD 2011 P-077 132 ------4. 3. dard deviation of0.46. stan- relative the with 99.99% as found was tablet in factor recovery sample.The pharmaceutical commercial in ycyline The same method was also applied to determination of dox gion for a concentration range of 0.05 to 0.5 mM (R re linear has electrode MIP at doxycyline for curve bration solution prepared in 30% acetonitrile-water at pH 2. The cali- buffer Britton-Robinson in obtained was electrode MIP with doxycycline towardof signaldoxycyline. anodic highest The The MIP electrode exhibited a high and selectivity sensitivity 4.0. and 1.5 pH the between mixtures binary nitrile-water The detection limit was determined as 4.24 x 10 x 4.24 as determined was limit detection The cline intabletat MIPelectrode. Figure.1. Differential pulse voltammogram for 1mM doxycy Kurzawa M., Kowalczyk-Marzec A. Electrochemical deter Electrochemical A. Kowalczyk-Marzec M., Kurzawa Masawat P., Mark Slater J. The determination of tetracy of determination The J. Slater P., Mark Masawat 2004. 95-102, 34: Analysis Biomedical and Pharmaceutical of Journal drugs. veterinary in oxytetracycline of mination 132, 2007. 127- 124: ActuatorsB and Sensors (SPGE). electrode gold screen-printed disposable a using food in residues cline i / A -0.10x10 -0.05x10 0.05x10 0.10x10 0.15x10 0.20x10 0.25x10 0.30x10 0.35x10 0.250 -3 -3 -3 -3 -3 -3 -3 -3 -3 0 0.500 0.750 E / V / E DPV 1.000 1.250 -5 M (S/N=3). M 2 =0.9997). - - - - - POSTER PRESENTATIONS - R (ATCC (ATCC 2 Staphy ) 3 3 3 2 , 4-OH 1 3 R Enterococcus Enterococcus 4-NO 4-OCH 3-OCH 4-N(CH 2 H 3-OCH C Bacillus subtilis Bacillus H C N 3 Vi Vj Vh Vg Vm (ATCC (ATCC aeroginosa Pseudomonas Com. H N Candida Candida albicans (ATCC 10231) and (ATCC 7002/ isolated isolated 7002/ (ATCC mirabilis Proteus N (RSKK 02026/ isolated strain), 3 1 H R O 4-F 2-Cl 4-Cl 4-Br C 4-CH N 2 H , Berrin ÖZÇELİK 2 N C (ATCC 29212/ isolated strain) ve ve strain) isolated 29212/ (ATCC - Aci strain), isolated 574/ (RSKK pneumoniae Klepsiella Vf Vc Ve Va Vd Vb Com. O (ATCC 25922/isolated strain), strain), 25922/isolated (ATCC strain), isolated 10145/ strain), netobacer baumannii lococcus lococcus aureus 25923/ (ATCC isolated strain), faecalis 6633/ isolated strain), 6258). krusei (ATCC Candida - - - - - 133 P-078 DRD 2011 DRD Mehtap GÖKÇE , Mehtap 1 Escherichia coli H-NMR spectra and 1 HYDRAZONE DERIVATIVES Zeynep ÖZDEMİR Zeynep International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International )-PYRIDAZINONE-2-ACETYL-2-(P-SUBSTITUTED BENZAL)

Gazi University, Faculty of Pharmacy, Department of Microbiology, 06330 Ankara, Türkiye Ankara, 06330 Department of Microbiology, of Pharmacy, Faculty Gazi University, 3 H

he pyridazinone nucleus has been incorporated into a wide variety of therapeutically interesting molecules to transform them into better drugs. 3(2 Due to favorable presence a pyridazinone moiety in moiety pyridazinone a presence favorable to Due Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06330 Ankara, Türkiye 06330 Ankara, Chemistry, Department of Pharmaceutical of Pharmacy, Faculty Gazi University, 2 İnönü University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 33169 Malatya, Türkiye 33169 Malatya, Chemistry, Department of Pharmaceutical of Pharmacy, Faculty İnönü University, 1

SYNTHESIS AND ANTIMICROBIAL OF EVALUATION 6-SUBSTITUTED- T elementary analysis. Antimicrobial activities of the synthe sized sized compounds were investigated against Some of the present day drugs such as emorfazone (analgesic), pimobendan (positive inotropic, vasodilator), - levosi zardav (cardiotonic), imazodan sensitizer), (calcium mendan erin (cardiotonic) medazonamide (antitussive) are the best examples for potent molecules possessing nucleus. pyridazinone known active structures, pyridazinone derivatives provoked a special interest in the search for new antibacterial agents Also, it is well known that the group hydrazone plays an im- hydrazone activityof number a antimicrobial the portant for derivatives have been claimed to possess interesting - anti bacterial and antifungal activities we re Considering above, H)-pyridazinone-2-6-substituted-3(2 eleven of synthesis port acetyl-2-(p-substitutedbenzaldehyde)hydrazone derivatives by the condensation reaction of H)-pyr 6-substituted-3(2 idazinone-2-acetohydrazides with substituted benzalde hyde derivatives. The structures of these new pyridazinone derivatives were confirmed by their IR, POSTER PRESENTATIONS rd, epciey Eetohmcl eair f ciprofloxa- of behavior Electrochemical respectively. trode, elec graphite pencil a on (ciprofloxacin) molecule template a without and with electrolyte supporting of presence the in (pyrrole) polymer conducting of deposition voltammetric werepolypyrrole electrodes (NIP) printedprepared bycyclic imprinted [5]. based onmolecularly polymer electrodes sensor a developed we fast and easy ciprofloxacin nolones qui- of member a of detection Tomake [4]. animals food in to define any risk to public health from the use of quinolones necessary is It [3]. infections systematic of treatment the for suitable are drugs these and antibiotics interestinggroupof most a comprise Quinolones [2]. drugs of determination the for used been have polymers imprinted stabilities, chanical sensors [1]. Owing to the high affinities, selectivities and me solid phase extraction, and as a selective electrophoresis,sorbent in chemical capillary chromatography, liquid as such methods, analytical several in applied been haveMIPs ence, 3. 2. 1. I Barbosa J, Barrón D, Cano J, Jiménez-Lozano E, Sanz-Ne E, Jiménez-Lozano J, Cano D, Barrón J, Barbosa preparation Electrochemical Y. Şahin M, Şahin L, Özcan and Developments imprinting: Molecular LI. Anderson n hs td, oeual ipitd MP ad non-im- and (MIP) imprinted molecularly study, this In methodologies for determing pKa values of quinolones of values pKa determing for methodologies absorptiometric and potentiometric chromatographic, bot V, Toro I. Evaluation of electrophoretic method versus 8:5792-5805,2008. Sensors acid. ascorbic of determination for electrode graphite pencil polypyrrole-modified imprinted molecularly a of Chro J matogr B745:3-13,2000. field. chemistry analytical the in applications REFERENCES new analytical techniques. In analytical seperation sci- seperation analytical In techniques. analytical new have gained and increasing interest in the research into (MIPs) polymers imprinted molecularly years, recent n CIPROFLOXACIN IN THE ACETONITRILE-WATER BINARY MIXTURE BINARY ACETONITRILE-WATER THE IN CIPROFLOXACIN Süleyman Demirel University, Faculty ofScience andArt,Dept.ofChemistry, Isparta, Türkiye ELECTROCHEMICAL BEHAVIOR AND QUANTIFICATION OF OF QUANTIFICATION AND BEHAVIOR ELECTROCHEMICAL Berrin GÜRLER International Symposium onDrugResearch &Development 2011 * , Sabriye PERÇİNÖZKORUCUKLU, EsengülKIR * [email protected] DRD 2011 P-079 134 - - - - obtained as70%(RSD0.052). was factor recovery The tablet. commercial in ciprofloxacin forused wasdeterminationof also electrode MIP (S/N=3). M of detection of ciprofloxacin was calculated to be 4.61 x 10 x 4.61 be to calculated ciprofloxacinwas of detection of limit The electrode. MIP at 0.991 of coefficient correlation a ciprofloxacinwith of mM 0.5-2 of range the curve in obtained was Calibration electrodes. NIP for than electrodes MIP for higher are ciprofloxacin of currents peak DPV The (DPV). voltammetry puls differential by 7.5 pH at mixture binary Robinson buffer solution prepared in 40% acetonitrile-water Britton- in investigated was electrodes MIP and NIP on cin 5. 4. ÖzcanŞahinY.L, paracetamolon of Determinationbased VoltammetricG. Y, Şahin Alsancak S, Özkorucuklu Perçin tors B127:362-369,2007. - Actua and Sensors electrode. graphite pencil modified polypyrrole imprinted electropolymerized-molecularly 8: 8463-8478,2008. overoxidized imprintedSensors polypyrrole. molecularly electropolymerized- on sulfamethoxazole of behaviour Biomedical Analysis 24:1087-1098,2001. and Pharmaceutical of Journal mixtres. hydroorganic in Figure. ofciprofloxacin. 1:Chemicalstructure -2

POSTER PRESENTATIONS - Effect of cream type product. cleansing Effect of cream 1b. Figure t-test. Student using statistically compared were data The Figure 1a. Effect of solution type cleansing product. Figure make-up remover: conditions of formation and its cleans- its and formation of conditions remover: make-up 43: 21-36, 1992. Chem J Soc Cosm ing mechanisms. Suzuki T, Nakamura M, Sumida H, Shigeta A. Liquid crystal Liquid A. Shigeta H, Sumida M, Nakamura T, Suzuki creased creased to 142 siemens due to enhanced dryness. This is in the claim of the product. to contrast - prod type cream that out found was it study, the of end the In ucts raised sebum levels slightly and increased the moisture levels from 237 microsiemens to 522 microsiemens. On the reduced products cleansing type solution of use hand, other sebum level The significantly. moisture level of the skin de 2. 135 P-080 DRD 2011 DRD [email protected] * ed: MA, USA: th Nefise Özlen ŞAHİN Nefise Özlen Atlan YÜKSEL, , Özge ŞAHİN, * International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Leman ÇELİK Leman

leaning products used for skin care belong to the group of frequently consumed cosmetic - prepa rations with the least known structure. Among

TURKISH MARKET ON SEBUM & MOISTURE LEVELS OF THE SKIN INVESTIGATING THE INFLUENCE OF CLEANSING FORMULATIONS IN - com cosmetic leading of products cleansing the Initially, The The purpose of use of these products is to intensively Chemical Publishing company, 2000. company, Chemical Publishing REFERENCES

Rieger MM. [ed]. Harry’s Cosmetology. 8 C Türkiye Campus, 33169 Mersin, Yenişehir Biopharmaceutics, Department of of Pharmacy, Faculty University, Mersin panies were selected and collected from the market to be tested. Next, the salon tests required for cream and tion type solu- cosmetics carriedwere out on The these products. test products were applied onto forehead and cheek of the healthy volunteers (n= 40) in the age range of 25 to 50 after obtaining their written consent for participation to this study. Sebum and moisture levels were measured before 1]. [Figure and after applying cleansing formulations clean the skin without interfering its properties. In literature, skinthe clean interfering without properties.Inits literature, it’s suggested that this type of products usually moisturize the skin as well as remove the sebum layer without caus- ing dryness and loss of moisture unlike traditional cleansing 2. soaps it However, seems difficult to support this claim for the marketed products. this Taken into consideration, in this study, the marketed cleansing products in the forms of creams and solutions were tested for their influence on the skin and sebum levels. moisture them, facial cleansing tissues, gels, milks, and single or multiple phase cleaning solutions are the most cleansing products1. widely used 1. POSTER PRESENTATIONS 3. 2. nephropathy1. diabetic and infarction, myocardialfailure, heart congestive of management the as such drugs these for emerging are to treat butadditionaltherapeutic hypertension, indications 1. the pK of determination for study number limited a are there But, established2. excretionbe percentagethe can and profile distribution the rate, absorption the nistration, the different acid–base species, the best way of drug admi- and structure the knowing Moreover, portance. im- pharmacological great a has drug tihypertensive ACETONITRILE-WATER BINARY MIXTURES BY POTENTIOMETRIC METHOD POTENTIOMETRIC BY MIXTURES BINARY ACETONITRILE-WATER Department ofChemistry, Faculty ofScience andLiterature, Süleyman Demirel University, 32260Isparta, Türkiye S Toscoa P, Rolando B, Fruttero R Henchoz Y, Martel S, Car S, HenchozY, Toscoa R Martel P,FrutteroB, Rolando Cagigal E, González L, Alonso RM, Jiménez RM. pKa deter J detailed study of ionization constants and distribution distribution and constants ionization of study detailed A sartans: of profiling Physicochemical A. PA, Gasco rupt 2001. byspectrofluorimetry. AnalPharmBiomed 477-486, J 26: II) (ARA antagonists receptor II angiotensin of mination Limbird, McGraw-Hill, 2001,New York. E. L. Hardman, G. J. Eds. TherapeuticsL, of Basis logical REFERENCES an- this of equilibria acid–base of knowledge The ackson EK, in Goodman and GilmanLs. The Pharmaco The GilmanLs. and Goodman in EK, ackson DETERMINATION OF DISSOCIATION CONSTANTS OF VALSARTAN IN VALSARTAN IN CONSTANTSOF DISSOCIATION OF DETERMINATION a 2-4. values ofvalsartan AT1 receptors. This antagonism is commonly used commonly is antagonism AT1receptors.This angiotensinantagonistsof (ARA-IIs) II atthe lective se as acting drugs of class important arean artans

International Symposium onDrugResearch &Development 2011

pK Macro-equilibria of valsartan ionization ofvalsartan Macro-equilibria Ebru ÇUBUKDEMİRALAY a1

[email protected] DRD 2011 P-081 136 - - - - are given in Figure. The pK Figure.The in given are valsartan of pathways Dissociation ring. tetrazole the and group acid carboxylic the centers, acidic two ins conta- 4-yl]methyl}-valine) (1H-tetrazol-5-yl)biphenyl- N-{[2_- ((S)-N-valeryl- Valsartan valsartan. of constants dissociation of determination the to method ometric . The aqueous pK aqueous The program5. PKPOT the using method potentiometric the by obtained valsartan of constants 40-60%) by using (R(v/v), potentiometric method. Dissociation interval the in mixtures acetonitrile-water in values predicted by ACD Sketch. Lab, Marvin us medium for have valsartan been compared with the agreement withACD Sketch programs. Lab, Marvin values of valsartan obtained from this study are in good 5. 4. Barbosa J, Barron D, Beltran JL, Sanz-Nebot V. PKPOT A PKPOT V. Sanz-Nebot JL, Beltran D, Barron J, Barbosa CombinedSA. ÇubukDemiralayEÇ, B,Özkan G, Alsancak The aim of this work is the application of potenti- of application the is work this of aim The Dissociation constants of valsartan are determined are valsartan of constants Dissociation 75-81, 1995. in aqueous and non-aqueous media. Anal Chim Acta 317: equilibria ionic of study potentiometric the for program age forms. JPharm BiomedAnal 53:475-482,2010. dos- pharmaceutical in determination their of timization op and antagonistsreceptor II angiotensin some of iour andpHonthechromatographiceffect ofpolarity behav coefficients. 91:468-482,2008. HelvChimActa pK a2

a values obtained in aqueo in obtained values - a - -

POSTER PRESENTATIONS - - - - C. The values o a 3 values obtai- a is based on the a values have been a Sibel A. ÖZKAN , Sibel A. 2 values determined in aceto a Hale CANBAY , Hale calculator, ACD Lab, MarvinACD Lab, Sketch. calculator, pK a 1,* Benzimidazoles are considered weak base. Two pro Two base. weak considered are Benzimidazoles dazole dazole derivatives by capillary electrophoresis. J Sep Sci 32: 1087-1095, 2009. omeprazole in aqueous solutions. Anal Chim Acta 481: 155-164, 2003. Yang Yang R, Schulman GS, Zavala Acid-base JP. chemistry of of these compounds were also determined potentio metrically. It is satisfying to note that pK equilibrium reaction benzimidazole of and protonated 2. Law Beer’s Benzimidazole and its derivates have limited solubility in water. In this work, acetonitrile water binary mixtures used to facilitate solubility of the benzimidazoles. tonation contants related to the protonations at the pyridine nitrogen and 3-position benzimidazole nit rogen atom and dissociation constant related to the deprotonation at the 1-position of the benzimidazole ring have been The 3. determined effect of the electron donating or withdrawing nature of these substituents were The investigated. aqueous pK nitrile The water results mixtures. obtained have been compared with the values predicted by on- the SPARC line pK hod, spectral data at different pH values were recorded recorded were values pH different at data spectral hod, over the wavelength region 198 - 346 nm at 25 method used for calculating the pK calculated calculated from the pK ned by the two methods are in close agreement. in close agreement. methods are the two ned by 3. - - Türkiye 137 P-082 DRD 2011 DRD [email protected] * VALUES OF PROTON PUMP INHIBITORS IN a values of benzimi- a K p Ebru ÇUBUK DEMİRALAY , Ebru ÇUBUK 1 ACETONITRILE BINARY WATER MIXTURES International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International The The PPI products contain this basic

Ankara University, Faculty of Pharmacy, Department of Analytical Chemistry, 06100 Ankara, Türkiye 06100 Ankara, Chemistry, Analytical Department of of Pharmacy, Faculty University, Ankara Merve GÜRKAYNAK Merve roton roton pump inhibitors (PPI) are used for the treatment of conditions such as ulcers gastroesophageal reflux and disease which are all 3 SPECTROSCOPIC

Süleyman Demirel University, Science & Literature Faculty, Department of Chemistry, 32260 Isparta,Türkiye of Chemistry, Department Faculty, & Literature Science University, Demirel Süleyman 1 Süleyman Demirel University, Experimental and Observational Student Practice and Research Centre, Isparta, Isparta, Centre, and Research Student Practice and Observational Experimental University, Demirel Süleyman values of these compounds by spectroscopic met REFERENCES The benzimidazoles possess characteristic absorpticharacteristic- possess benzimidazoles The General structures of PPI.

The The PPI pharmacophore is 2-pyridylmethylsulfiny Determination Determination of thermodynamic pK A 70(5): 1-11, 2006. Educ J Pharm Am tors. Jerez G, Kaufman G, Prystai M, Schenkeveld S, Donkor KK.Donkor S, Schenkeveld M, Prystai G, Kaufman G, Jerez Victoria Victoria F. The chemically elegant proton pump inhibi- 2

a P on spectra in the UV region. In order to determine the pK 1]. lbenzimidazole caused by stomach acid. Omeprazole, lansoprazole, pantoprazole, and rabeprazole are the member of PPI. They have a smaller anti-secretory potency on a milli- basis. gram 2. 1. structural framework and differ only in the nature of benzimidazole and pyridine the on placed substituents rings. POSTER PRESENTATIONS 45%). Potentiometry has been the most useful techniques useful most the been has Potentiometry 45%). (30- mixtures binary methanol–water in potentiometrically or estimated by their pK their by estimated or behavi- protolytic their to related are PPI of characteristics cells.in the parietal of protonic activity The pharmacological reduction the to lead that reactions ionic of series a by ated initi- is similar.activity areTheir properties pharmacological their groups, benzimidazole the or pyridine the on titutions subs- different with benzimidazoles α-pyridylmethylsulfinyl closest properties to waterclosest properties 2. the shows recommended methanol solvents, organic the widely among because, been have mixtures binary water that ity forces the use of a hydro-organic solvent. Methanol- of aqueous pK determination the in water. in difficulty main the often, Very dissolve to difficult very is it therefore, molecule, non-polar 2. 1. DETERMINATION OF OF DETERMINATION P 2 Ruiz R, Rosés M, Ràfols C, Bosch E. Critical validation of validation Critical E. Bosch C, Ràfols M, Rosés R, Ruiz Jerez G, Kaufman G, Prystai M, Schenkeveld S, Donkor Donkor S, Schenkeveld M, Prystai G, Kaufman G, Jerez POTENTIOMETRIC METHOD IN METHANOL-WATER BINARY MIXTURES BINARY METHANOL-WATER IN METHOD POTENTIOMETRIC n hs td, pK study, this In a new simpler approach to estimate aqueous pK aqueous estimate to approach simpler new a 32:1087-1095,2009. Sci Sep J electrophoresis. capillary by derivatives imidazole KK. DeterminationKK. of thermodynamic pK REFERENCES Süleyman Demirel University Experimental andObservational StudentPractice andResearch Centre, Isparta, 1 Süleyman Demirel University, Science &Literature Faculty, DepartmentofChemistry, 32260Isparta, Türkiye Te are secreti- They ulcers 1. acid peptic of gastric treatment for and on of inhibitor be effective to shownan have (PPI) inhibitors pump roton İsmail ÇELİK a of drug candidates is their aqueous insolubil- a aus f P hv be determined been have PPI of values a values. Benzimidazole is a slightly a is Benzimidazole values. International Symposium onDrugResearch &Development 2011 1 , Güleren ALSANCAK p K a VALUES OF BENZIMIDAZOLE DERIVATIVES WITH WITH DERIVATIVES BENZIMIDAZOLE OF VALUES a values of benz- * [email protected] DRD 2011 1,* P-083 , EbruÇUBUKDEMİRALAY 138 Türkiye a

ment of equilibrium constants allows the different pK refine the for program computer of use the Moreover,lity. reproducibi- and hydro- accuracy their of because mixture, organic in constants equilibrium of determination the for tor, ACD Sketch. Lab, Marvin 3. analysis of the chemical structure. The pK The structure. chemical the of analysis eous pK eous sociation canalsobeevaluated. most important solvent properties that affect electrolyte dis- the and found relationships the from calculated be can ture in polyprotic substances3. (π*, α, β). The pK The β). α, (π*, parameter solvatochromicTaft and Kamlet the with related cor were mixtures methanol-water in studied PPI four the with the values predicted by the SPARC on-line pK SPARCon-line the by predicted values the with compared been have pantoprazole for medium aqueous in Barbosa J, Barron D, Beltran JL, Sanz-Nebot V. PKPOT A PKPOT V. Sanz-Nebot JL, Beltran D, Barron J, Barbosa 75-81, 1995. in aqueous and non-aqueous media. Anal Chim Acta 317: equilibria ionic of study potentiometric the for program 210-221, 2005. 550: Acta Chim water.Anal in soluble sparingly drugs of cmltl dfeet prah t eaut te aqu- the evaluate to approachs different completely A pK The a of organic compounds are the one based on the on based one the are compounds organic of a values determined for the involved equilibria for involved equilibria the for determined values a values of PPI in any methanol-water mix methanol-water any in PPI of values 1 , Hale CANBAY a values obtained values 2 a calcula- a values - - - POSTER PRESENTATIONS - - Pseudomo -phenyl ring N-phenyl Enterococcus Enterococcus ) faecalis against two Gram posi- Gram two against ed., Vol 23, Wayne, PA: NCCLS, NCCLS, PA: Wayne, 23, Vol ed., in vitro vitro in th 1 Zeynep SOYER , Zeynep 2 2003. (2007). ARKİVOC XV : 112-126 antimicrobial dilution for Methods NCCLS) (Formerly CLSI susceptibility tests for bacteria that grow aerobically ap proved standard M7-A6, 6 M7-A6, standard proved

4. literature literature reviews, we aimed to synthesize ten - 2/3-(benzoyl amino)propionanilide derivatives bearing substituents with on electronicnature and liphophilic different spectral by confirmed were compounds of structure the and and elemental analysis. The target compounds were tested activity antimicrobial their for tive bacteria (Staphylococcus , aureus and bacteria two Gram negative , (Escherichia coli 4. method (CLSI) using microdilution ) by nas aeruginosa - 139 P-084 DRD 2011 DRD , Bayri ERAÇ 57: 1528- *[email protected] 1, * Şirin UYSAL International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME 2/3-(BENZOYLAMINO)PROPIONANILIDE DERIVATIVES

he usage of most antimicrobial agents is limited resistance drug developing rapidly the by only not but also the increasing resistance of pathogene

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege Unıversity, 35100 Bornova, İzmir, Türkiye İzmir, 35100 Bornova, Unıversity, Ege of Pharmacy, Faculty Chemistry, Department of Pharmaceutical

1 T 1538, 2005. REFERENCES Narasimhan Narasimhan B, Narang R, Judge V, Ohlan R, Ohlan S. Black MT, Hodgson J. Adv Drug Delivery Rev Koehn FE. J MedKoehn FE. Chem 51: 2613-2617, 2008. Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Ege Unıversity, 35100 Bornova, İzmir, Türkiye İzmir, 35100 Bornova, Ege Unıversity, of Pharmacy, Faculty Microbiology, Department of Pharmaceutical 2 3. 2. 1. organisms organisms and side effects. Therefore, there is still need to develop new antimicrobial compounds which enhances ac tivity profile. Literature data shows that substituted anilides have a wide range of bioactivities such as antimicrobial, antifungal, anticonvulsant, anaesthetic, antiproliferative, - anti potassium and antioxidant antiplatelet-aggregation, plaque, channel activating 1-3. potentials In this study, based on the POSTER PRESENTATIONS hydrophobicity oftheseanalogues2. growing with correlated ligands, amine hydrophobic more cisplatin analogues, in which NH which in analogues, cisplatin of increasing cytotoxicity thatshown been has anologues.It the of effects biological of character the affect may which DNA, target in alterations formational and structural rent reduced toxicity. and efficacy, clinical improved activity, of spectra broader with analogues cisplatin developing to devoted been have efforts tremendous far, So cancers. some in cisplatin of use the limit effects side toxicity.These and resistance acquired agent, cisplatin exhibits two main disadvantages: intrinsic or cell lung cancer1. testicular ovarian, bladder, cervical, small-cell and non-small- for treatment of mainstay the is cisplatin 1967, in cisplatin 1. 2. SYNTHESIS AND CHARACTERIZATION OF PLATINUM(II) COMPLEXES WITH WITH COMPLEXES PLATINUM(II) OF CHARACTERIZATION AND SYNTHESIS Rosenberg B, Van Camp L, Krigas T. Inhibition of cell di- cell of Inhibition T. Krigas L, Camp Van B, Rosenberg Tallen G, Mock C, Gangopadhyay SB, Kangarloo B, Krebs B, Kangarloo SB, Gangopadhyay C, Mock G, Tallen The replacement of ammine groups can result in diffe in result can groups ammine of replacement The chemotherapeutic a as application wide its Despite of activity antitumor the discovered Rosenberg Since iin in vision REFERENCES B, Wolff JEA. Overcoming cisplatin resistance: Design of Design resistance: cisplatin Overcoming JEA. Wolff B, platinum. Nature electrode 205:698-699,1965. 1 Mersin University, Faculty ofPharmacy, Dept.ofPharmaceutical Chemistry, 33169Mersin, Türkiye 2 GaziUniversity, Faculty ofPharmacy, Dept.ofPharmaceutical Chemistry, 06330Ankara, Türkiye shrci coli Escherichia IMIDAZOLE AND 2-PHENYLIMIDAZOLE LIGANDS 2-PHENYLIMIDAZOLE AND IMIDAZOLE International Symposium onDrugResearch &Development 2011 Semra UTKU y lcrlss rdc fo a from product electrolysis by 3 groups were replaced by replaced were groups 1 , ÇağlaBOĞATARKAN * [email protected] DRD 2011 P-085 140 - hrceie b ter lmna aaye, IR, analyses, elemental their by characterized and synthesized were groups) “non-leaving as limidazole ESI-LC/MS. molecules including iron-heme systems, vitamin B vitamin systems, iron-heme including molecules important biologically of variety a in ions metal transition towardligands as moiety,function histidine a as ligand, tive pounds as ligands. The imidazole ring is a physiologically ac com- active physiologically use to is drugs anticancer num tures derivatives andseveral metalloproteins3. 3. Sundberg R, Martin RB. Interactions of histidine and other n ntwrh apoc i te ein f e plati- new of design the in approach noteworthy One In this study, four platinum(II) complexes with the struc the with complexes platinum(II) fourstudy, this In cal andbiological systems. 74:471-517,1974. ChemRev imidazole derivatives with transition metal ions in chemi- 20: 445-450,2000. novel hydrophobic platinum compounds. Anticancer Res cis-[PtL 1, * , Fatma GÜMÜŞ 2 Cl 2 and ] cis-[PtL 2 I 2 2 (=mdzl o 2-pheny or (L=imidazole ] 1 NR and NMR H 12 and its and - - - POSTER PRESENTATIONS - - 1 Emel D. KURTOĞLU , Emel D. 1 2 Berrak GÜNEY , Berrak trimetazidine in plasma samples for assessing bioequiv alence of immediate/modified 2005. 19: 549-555, Biomed Chromatogr release formulations. MS–MS for the determination of trimetazidine in human 71: 1101-1105, 2010. plasma. Chromatogr The sample preparation based on liquid-liquid extraction liquid-liquid on based preparation sample The Zhang T, Meng P, Kou W Zhang Meng T, et P, al. Rapid and sensitive UPLC- 1 3. matographically matographically separated on Sunfire Waters a C18 column, (2.1 x 50 mm, 3.5µm) with the mobile phase consisting of methanol, water and formic acid (500:500:1, v/v/v) at a flow rate of The 0.2 calibration curvesmL/min. linear were within (LOQ) quantification of limit The ng/mL. 2.5-250 of range the was 2.5 ng/mL. This method was successfully aplied to the pharmacokinetic study of trimetazidine in healthy - volun teers. with ethyl acetate using 0.2 mL human plasma. Tizanidine was used as the internal standard. The analytes were chro - - - 141 P-086 DRD 2011 DRD Tuncel ÖZDEN , Tuncel [email protected] * , Suna TOPTAN 1 Novagenix Bioanalytical Drug R&D Centre, Ankara, Türkiye Ankara, Drug R&D Centre, Bioanalytical Novagenix 1 , Sami EREN 1,* International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Türkiye Ankara, Chemistry, Department of Pharmaceutical of Pharmacy, Faculty Gazi University, rapid liquid chromatography electrospray - ioniza electrospray liquid rapid chromatography with method spectrometrymass (LC/ESI-MS) tion good sensitivity and specificity has been - devel 2

Nesrin YÜZÜAK Nesrin QUANTIFICATION OF TRIMETAZIDINE IN HUMAN PLASMA BY LIQUID REFERENCES Medvedovici Medvedovici A, Albu F, Georgia C, David V. Non-extrac hensive hensive review of the pharmacological effects and analytical techniques the for determination of trimetazidine. 2008. 26(2): 147-165, Ther Cardiovasc tive procedure followed by LC/APCI MS/MS analysis of Trimetazidine Trimetazidine is a anti-ischaemic drug, which protects Beşikçi OA, Özkan revisited: Trimetazidine SA. A compre

A CHROMATOGRAPHY-ELECTROSPRAY IONIZATION MASS SPECTROMETRY 1. 2. the myocardial cell from the harmful effects of ischaemia1,2. Trimetazidine was used for the treatment of angina pecto oped and validated for the of quantification trimetazidineoped for and in validated human plasma. ris, ris, ischemia in the neurosensorial dis- tissues and Meniere’s ease3. POSTER PRESENTATIONS chemical methods8,9. electro and optical6 electrophoresis5, capillary tography4, chroma- liquid high-performance as, such determination: DNR for synthesis2. methods instrumental numerous acids been have There nucleic inhibite can it therofore bonds; hydrogen damage and bases (C) Cytosine and G between intercalate structure, base (G) Guanine destroy can It agent. chemotherapy as treatment leukemia for used is it that otic, oftechniques1-3 includingelectrochemistry.variety a by studied been have DNA with drugs anticancer some of interactions the Therefore, compounds. carcinogenic some 5. 4. 3. 2. 1. [5] free of determination Simultaneous I.. Morita S, Emara sensing electrochemical based Nanomaterial A. Erdem Badner X, Wu SJ, Shukla RS, Huang WK, Bleibel S, Duan, and hybridization DNA Detecting M. Fojta E., Palecek Daunorubicin (DNR) is an anthracycline anticancer antibi- 1973–1979, 1994. 41: Talanta pre-columns. protein-coated column-switching and technique using plasma in duanorubicin adriamycinone and adriamycinol, adriamycin, bound and strategies. Talanta 74:318-325,2007. 2007. Res Cancer cytotoxicity. rubicin-induced dauno to contribute that genes Mapping ME. Dolan JA, 73:74A-83A, 2001. damage. Analytical Chemistry REFERENCES tumor. JChromatogr A853:449-455,1999. sarcoma Kaposi in daunorubicine of analysis the to tion electrophoresis: Applica - analysis bythracycline capillary T VOLTAMMETRIC AND IMPEDIMETRIC DETECTION OF INTERACTION INTERACTION OF DETECTION VOLTAMMETRICIMPEDIMETRIC AND Simeon N, Chatelut E, Canal P, M, Couderc Nertz F. An- im f cin f niuo, niia dus and drugs antiviral antitumor, of action of nism mecha- the understanding for importance great a has interactions drug–DNA on investigation he BETWEEN ANTICANCER DRUG DAUNORUBICIN AND DNA DNA AND DAUNORUBICIN DRUG ANTICANCER BETWEEN Ege University, Faculty ofPharmacy, DepartmentofAnalytical Chemistry, İzmir, Türkiye International Symposium onDrugResearch &Development 2011 Gülşah ÇONGUR,Ayfer ÇALIŞKAN, ArzumERDEM 67: 5425–5433, 67: * [email protected] DRD 2011 P-087 142 - - interaction process, the charge transfer resistance (R after and Before technique. DPV using by response sensor the on based studied were time interaction DNR-DNA and concentration DNA concentration, DNR as such parameters oxidation signals of DNR and guanine. Effect of experimental the at changes the monitoring by voltammetrically tigated inves- was DNA with DNR of interaction phase. The solution and also in the double stranded DNA surface both electrode and DNR between methods interaction of monitoring for used (EIS) were spectoscopy impedance electrochemical sociate memberof TUBA for theirsupport. as- the as (TUBA) Sciences of AcademyTurkishthe to titude under theseoptimumconditions. was measured byned at surface the EIS electrode technique 9. 8. 7. 6. re A Krdnz , aıkn . edie modified Dendrimer A. Çalışkan H, Karadeniz A, Erdem carbon Single-walled A. Çalışkan H, Karadeniz A, Erdem Hu Q, Zhang L, Zhou, T,L, FangZhang Q,dauno Y. Hu of Determination Ad- P, Bartak P, Bednar J, Psotova J, Sevcik A, Gavenda n hs td, ifrnil us vlamty DV and (DPV) voltammetry pulse differential study, this In A.E would like to express her gra- her express to like would A.E Acknowledgements: spectroscopy. Analyst 136:1041-1045,2011. impedance electrochemical and voltammetry by rubicin graphite sensors for of anticancer detection drug dauno interactions. Electroanalysis 21:464-471,2009. biomolecular and acids electro nucleic of monitoring for chemical electrodes graphite modified nanotubes 19, 2000. 15- 416: Acta Chim. Anal. detection. amperometric with electrophoresis zone capillary by urine human in rubicin phoresis 22:2782-2785,2001. Electro detection. absorption UV with electrophoresis capillary by daunorubicin and doxorubicin antibiotics anthracycline of Determination V. Simanek P, amovsky * ct ) obtai- - - - - POSTER PRESENTATIONS - - Mitomycin C Mitomycin * In our study, carbon nanotube-biopolymer composite - grati her express to like would A.E Acknowledgements: nanotubes modified graphite electrodes for electro chemical monitoring of nucleic acids and biomoleculer 2009. 21: 464-471, Electroanalysis interactions. tion on the single-walled carbon nanotubes modified sensors detected by voltammetry and electrochemical impedance spectroscopy. Electroanalysis 21: 2116-2124, 2009. Karadeniz H. Streptavidin modified carbon specific sequence label-free electrode for based graphite nanotube DNA detection. 22: 611-617, 2010. Electroanalysis Erdem Erdem A, Karadeniz H, Çalışkan A. Single walled carbon Çalışkan A, Karadeniz H, Erdem A. Direct DNA - hybridiza Erdem A, Papakonstantinou P, Murphy H, Mcmullan M, troscopy (EIS) techniques. troscopy electrode was developed for electrochemical monitoring of pulse differential using by DNA and MC between interaction voltammetry (DPV) and electrochemical impedance spec tude to the Turkish Academy of Sciences (TUBA) as the as- their support.TUBA for member of sociate 6. 7. 8. - - - - 143 P-088 DRD 2011 DRD 78: 6656- [email protected] * MITOMYCIN C AND DNA . 4 , Arzum ERDEM CANAVAR Ece Pembe caespitosus Streptomyces , can be combined with classic International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International 4-8 . 1-4 Türkiye İzmir, Department, Chemistry Analytical of Pharmacy, Faculty Ege University,

NA biosensors play an important role in the new generation sensor technology with a wide range of These application biosensors areas. has - recog

FOR ELECTROCHEMICAL MONITORING OF INTERACTION BETWEEN nomycin nomycin and its interaction with double-stranded and single-stranded DNA adsorbed at the electrode. Bioelec 17: 7-14, 2005. Electroanalysis sors. damage. Analytical Chemistry Analytical damage. 2001. 73: 74A-83A, 2007. 74: 318-325, Talanta ing strategies. REFERENCES trochemistry 55: 165-167, 2002. bridization at Disposable Graphite Electrodes Modified with Carbon Nanotubes. Analytical Chemistry 6659, 2006. Today Today nanomaterials in different properties have been Mitomycin C (MC) an antitumor agent and anticancer anti anticancer and agent antitumor an (MC) C Mitomycin Erdem A, Papakonstantinou P, Murphy H. Direct DNA Hy Erdem A, P, Papakonstantinou Jelen F, Jelen Erdem F, A, Palecek E. Cyclic voltammetry of echi- biosen- electrochemical based Carbon-nanotube J. Wang Palecek Palecek E, Fojta M. Detecting DNA hybridization and sens- DNA electrochemical based Nanometarial A. Erdem D CARBON NANOTUBE-BIOPOLYMER COMPOSITE MODIFIED ELECTRODES sensor technology. Especially composite structure formed by carbon nanotubes and various polymers can be used for of the sensor surfacethe modification 5. 2. 4. 1. 3. still under development nition surfaces which are formed of nucleic acid sequences, detect target based on nucleic acid hybridization which allows high selectivity in the in analysis. nucleic Recently, acid analysis, electrochemical DNA biosensors popular have with become their practicality, reliability, high sensitivity, fastness and economy biotic drug, which was isolated from from isolated was which drug, biotic used in the against chemotherapy anticancer a broad spec cancers. gastrointestinal for especially tumors, solid of trum POSTER PRESENTATIONS 6. 5. 4. 3. 2. 1. 11. activity antitumor has which of antibioticsThe mechanism resulting inefficient magnetic separation. as limits detection low exceedingly in observed bridization hy DNA of detection spesific sequence the brings ticles8, nanopar metal with combining or system4,9-10 free label ing 7 or - us 4,6-10 as labeling with an enzyme on magnetic particles the nitrogenous basesofDNA5,6. with complexes form which etc.) complexes, coordination metal antibiotics, (some intercalators DNA using or adenine guanine/ of signal oxidation the on based 3-4 directly events hybridization exploitedbe for monitoringsequence-specific

D Karadeniz H, Erdem A, Kuralay F,F.Kuralay Jelen Indicator-based A, Erdem H, Karadeniz Echi - of voltammetry Cyclic E. Palecek A, F,Erdem Jelen Magnetic-beads M. Salazar A, Erdem AN, Kawde J, Wang Erdem A, Pividori MI, Del Vale M, Alegret S. Rigid carbon com Anal.damage. and hybridization DNA FojtaM. PalecekE, to biosensors DNA From summary: and Survey J. Wang lanta 78:187-192, 2009. Tasystem. - sensor acid nucleic electrochemical posable dis- with connected assays magnetic indicator-free and trochem 55:165-167,2002. Bioelec electrode. the at adsorbed DNA single-stranded and double-stranded with interacion its and nomycin bridization. Analyst 126:2020-2024,2001. hy DNA of detection electrochemical label-free based chemical genosensing. J Electroanal Chem 567: transducing 29-37, new label-free materialposites: for A electro2004. Chem 73:75A-83A, 2000. gene chips. NuclAcids 28:3011-3016,2000. Res cioyi (CI rpeet oe f h quinoxaline the of one represents (ECHI) Echinomycin based system sensor acid nucleic electrochemical The REFERENCES USING ANTITUMOR DRUG ECHINOMYCIN AS AN ELECTROCHEMICAL ELECTROCHEMICAL AN AS ECHINOMYCIN DRUG ANTITUMOR USING MAGNETIC-BEAD ASSAY FOR MONITORING OF DNA HYBRIDIZATION HYBRIDIZATION DNA OF MONITORING FOR ASSAY MAGNETIC-BEAD Ege University, Faculty ofPharmacy, Analytical Chemistry Department,35100Bornova, İzmir, Türkiye and these devices can devices these and environments1,2 various in agents infectious of diagnoses early determining NA hybridization biosensors can be employed for International Symposium onDrugResearch &Development 2011 Hakan KARADENİZ,ArzumERDEM *[email protected] INDICATOR DRD 2011 P-089 144 ------11. 10. 9. 8. 7. sociate memberof TUBA for theirsupport. as- the as (TUBA) Sciences of AcademyTurkishthe to titude DNAsequences.base mismatch andnoncomplementary hybridizationinvestigatedalso was presencethe single in of DNA for assays magnetic these of selectivity technique.The (DPV) voltammetry pulse differential using by hybridization DNA of presence the in monitored were adenine and nine gua- bases; DNA electroactive and indicator,ECHI of signals oxidation the at changes The hybridization. DNA de of tection electrochemical the for developed successfully were sensor, graphite disposable a with connected assays netic strong preference for theCpG sequence11. tion. It can bind to the minor groove of DNA duplex showing bisintercala- as described was dsDNA with interaction ECHI

Waring MJ, Wakelin LP. Echinomycin: A interbifunctional Erdem A, Pividori MI, Lermo A, Bonanni A, Del Valle M, Aleg P, Kara H, - Sa A, Karadeniz Ariksoysal, Şengönül A, Erdem Wang J, Liu GD, Merkoci A. Particle-based detection of DNA WangJ,Erdem PolskyA, Xu MA. DK, Salazar - R, Genomag calating antibiotic. Nature 252:653-657,1974. Sensors and Actuators B-Chemistry 114: 591-598, 2006. magneto-compositeelectrodes.usingdetection hemical electroc label-free on based assay Genomagnetic S. ret Electrochem CommunElectrochem 7:815-820,2005. technology.sensor disposable using by amplicons chain polymerase DNA in virus B Hepatitis of detection the for assay genomagnetic Electrochemical M. Özsöz AA, yıner ments of an iron tracer. Anal Chim Acta measure 482: 149-155, stripping electrochemical 2003. using hybridization ta 56:931-938,2002. netic assayselectrochemical of DNA hybridization. Talan- A.E would like to express her gra- her express to like would A.E Acknowledgements: mag- indicator-free and indicator-based an study, our In * - - - - - POSTER PRESENTATIONS - , 2 J. SOLEIMANI RAD , J. SOLEIMANI 2 2 It is concluded that tamoxifen suppresses follicular - dif Medlineplus Health Information Medical sources: Health Problems in Pregnancy- , L. ROUSHANGAR 1 tions, tions, the number of follicular nests, primordial and primary us- values with control and compared counted were follicles ing t-test. Morphometry and microscopy revealed that on 2nd and 3rd days, the follicular nests appeared as clusters of somatic or pre-granulosa cells surrounding oocytes. The number of follicular nests was significantly (p< 0.001) higher in experimental group in comparison to control group (20±1.49 vs 28.8±1.25) indicating suppression of follicular development in tamoxifen treated group. On the 6th and - fol primaryof multilayered number the infants, old days 7th licles were significantly (p<0.01) lower than those in control group 50.85±3.07 vs 62.88±3.33. However, most of the - fol primary state. in monolayer follicle licles were ferentiation and development at early stages of folliculo genesis which could in result depletion of ovarian reserve in adulthood1,2. 2. - - - 145 P-090 DRD 2011 DRD K. AFSORDEH Iran Sciences, of Medical [email protected] * , H. MAZUOCHIAN 1,* DIFFERENTIATION IN MICE FETAL OVARY International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International M. KARIMI SHOAR , M. KARIMI 1 TAMOXIFEN SUPPRESS FOLLICULAR DEVELOPMENT AND

ollicular nests is an early stage of follicular - devel opment which is not hormone dependent. Mecha- nisms regulating the development of primordial

R. PIRI Medical student, Student Research Committee, Faculty of Medicine, Tabriz University of Medical Sciences, Iran Iran Sciences, of Medical University of Medicine, Tabriz Faculty Committee, Student Research student, Medical REFERENCES urnal Center In this study 30 adult female and 15 adult male mice are Text sources: EBSCO, Ingenta OhioLINK plc, Electronic Jo EBSCO, sources: Text

1 F Neuroscience Research Center and Department of Histology and Embryology, Faculty of Medicine, Tabriz University University of Medicine, Tabriz Faculty and Embryology, Department of Histology and Center Research Neuroscience 2 1. vation vation of vaginal plaque was considered as the first day of pregnancy and the mice on 13th day of pregnancy received 100µgr Tamoxifen as ip injection. After delivery, 2, 3, 6 and 7 days old new borns were sacrificed and their ovaries were fixed and prepared for light microscopic studies. In the sec used. used. The female mice are divided into two groups of - con cycle estrous their at mice female Two experimental. and trol were put with one male mouse in a cage for mating. Obser follicles follicles and their transition to primary follicles are not well maternal if investigate to is study this of aim The established. treatment with tamoxifen, a drug which binds to estrogen receptors and is used for induction of ovulation and cancer development. follicular effect on fetal has any treatment, POSTER PRESENTATIONS ethers also showed remarkable anticonvulsant activity In the recent years, it has been reported that nafimidon oxime thisgroupstructuraloftheand requirements activity.forthe group sant drugs and nafimidone is one of the representatives of this popular.stillanticonvulis (Arylalkyl)imidazoles groupof a is these drugs seizurescontrolledthemoreovercannotbe of type someby and effectsundesirableside many have them of most since aticandnonethe ofantiepileptic drugs theinmarket idealis e SR ad o ban e atcnusn compounds. anticonvulsant new obtain to and SARs new establish to activities anticonvulsant their test to and esters 1. 3. 2. SYNTHESIS OF SOME NEW NAFIMIDONE OXIME ESTER DERIVATIVES AND AND DERIVATIVES ESTER OXIME NAFIMIDONE NEW SOME OF SYNTHESIS E aasa . e atcnusn agents. anticonvulsant New B. Malawska Karakurt A, Dalkara S, Özalp M, Kendi E, Stables JP.Syn- Stables E, Kendi M, Özalp S, Dalkara A, Karakurt Walker KAM, Wallach MB, Hirschfeld DR. 1-(Naphthylalkyl)- Therefore, in this study, we aimed to prepare some oxime REFERENCES ime and oxime ether derivatives and their anticonvulsant ox 1-(2-naphyl)-2-(imidazole-1yl)etanon some of thesis agents. JMedChem24:67-74,1981. anticonvulsant of class new a derivatives, 1H-imidazole Chem 5:69-85,2005 2 Hacettepe University, 2 1 . There are many articles in the literature about the SARs İnönü University, population.symptomAntiepileptictherapyis drug world’s the of number large a affects and diseases neurological common most the of one is pilepsy Mehmet AbdullahALAGÖZ 1 . Therefore to develop new anticonvulsant agents

Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 44280Malatya, Türkiye International Symposium onDrugResearch &Development 2011 O N

Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 06100Ankara, Türkiye O C H THEIR ANTICONVULSANT ACTIVITIES ANTICONVULSANT THEIR H 3 N B r 2 N D R C - C C O / D 1 O M , ArzuKARAKURT H ur o Med Top Curr A P 3 O . DRD 2011 P-091 C H 146 2 B - - - r H N TAK (Project No:11S270). to theoxime ethers3. in rotorod test. These activities were found to be comparable neurotoxicity showed compounds the of none and seizures ScM and/or haveMES done anticonvulsantaganist activities was evaluated by rotord test according to ASP4. compounds the of neurotoxicity and ip mice in tests (ScM) seizure metrazole subcutaneous and (MES) seizure shock electro maximal by determined were activities convulsant IR, by confirmed were compounds these of Structures oxime. nafimidone of esterification by synthesized were midone nafi- of derivatives ester oxime new three purpose this For 4. N 1 tbe J, ufreg J h NH niovlat drug anticonvulsant NIH The HJ. JP, Kupferberg Stables Acknowledgement: This Project was supported by TUBI - We found that all of the oxime ester derivatives of nafimi- 1997. Ltd; Company & Libbey John England: London, M. (Eds.), Avoli P, Tanganelli G, Avanzini drugs, antiepileptic for targets cellular and molecular in: project, screening anticonvulsant preclinical program: (ADD) development 2001. activities. antimicrobial and N H-NMR MASS and elementary analysis data. Their anti- Their data. analysis elementary and MASS H-NMR 1 O , ÜnsalÇALIŞ O N R N O R R R = = = 2

, Sevim DALKARA - - C C C H H H 2 2 ( C C H H N 2 3 C

( . 36: 421-433, 36: Chem. Med J Eur 1 H a 2 ) C N H 3 ) 2

( 1 N b ( H ) 1 c 2 O

) H . H C l 2 - POSTER PRESENTATIONS - S R N N N N n ) 2 H C ( O c 2 - a 1 3 H C S H N 2 H N N N ]-1,3,4-thiadiazine derivatives with pos with derivatives ]-1,3,4-thiadiazine * b n ) 2 H ]-1,3,4-THIADIAZINES C ( 2 , b O 1 l C -

, F -

, 2

H , - 1

: : Titled Titled compounds have been synthesized by reacting 3 R n -1,2,4-triazolo[3,4-

H H C Herein Herein we describe the synthesis of novel 3,6-disubstituted- 7 activity. anti-inflammatory/analgesic sible 4-amino-1,2,4-triazole-5-thiones with appropriate phenacyl bromides (or chlorides) in anhydrous ethanol under reflux and chemical structures of the compounds were confirmed spectral by data. - - - ]- b 147 P-092 DRD 2011 DRD *[email protected] -1,2,4-triazolo[3,4- H Birsen TOZKOPARAN , Birsen AYTAÇ S. Peri International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL

activities activities besides ulcer negligible risk in the stom

or treatment of inflammatory and rheumatic seases, di- nonsteroidal (NSAIDs) anti-inflammatory are still considered drugs as the first choice 3,6-DISUBSTITUTED 1,2,4-TRIAZOLO[3,4-

Almost twenty years, on the purpose of developing novel novel of developing on purpose the years, twenty Almost F Türkiye Ankara, 06100 Sıhhiye, Chemistry, Department of Pharmaceutical of Pharmacy, Faculty University, Hacettepe compounds carrying analgesic/anti-inflammatory activity, we we activity, analgesic/anti-inflammatory carrying compounds and he their condensed on have focused mercaptotriazoles ir gastrointestinal-focused adverse effects and renal toxicity risks are limiting their therapeutic usefulness. In this regard, still a necessity. are agents of safer development On studies the of basis our preliminary derivatives. terocyclic that some 3,6-disubstituted-7 showing among the various pharmacological groups. However, the 1,3,4-thiadiazine 1,3,4-thiadiazine derivatives had potent anti-inflammatory/ analgesic ach, ach, we have planned some further modifications. structural POSTER PRESENTATIONS 1. in both RMS and ES. Hence, in this work we aimed to ana- to aimed we work this in Hence, ES. and RMS both in efficiency treatment the improving for require in are egies remainspoor.disease still Therefore,novel therapeuticstrat metastatic with patients for outcome the therapy,radiation surgery,ing intensivedose combination chemotherapy, and incorporat approaches aggressive despite ES, and RMS in Both children. in observed cancer bone of form lethal most the is malignancy bone primary common most second the mors in patients under 15 years of age. Ewing’s sarcoma (ES), tu- malignant all of 5% for accounts and adolescence and childhood the of malignancies common most the among is (RMS) Rhabdomyosarcoma adults. in neoplasms all of 5% 1. of anti-tumour activities hypericinand flavonoids(HY) (quercetin) with a broad range and xanthones proanthocyanidins, (hyperforin), roglucinols phlo (hypericin), naphthodianthrones as such constituents interest. of centre the of effects the years recent In centuries1. for disorders psychiatric and S eia A Mríe-oea , mrsSnhz MI, Amores-Sánchez B, Martínez-Poveda MA, Medina bioactive compound?bioactive Life Sciences79:105–111, 2006. antidepressant an than More Hyperforin: AR. Quesada REFERENCES acms ersn 2% f eiti mlgace and malignancies pediatric of 20% represent Sarcomas ANTIPROLIFERATIVE AND APOPTOTIC EFFECTS OF OF EFFECTS APOPTOTIC AND ANTIPROLIFERATIVE inflammatory diseases, peptic ulcers, skin wounds skin ulcers, peptic diseases, inflammatory nal plant that has been used to treat respiratory and t. John’s L.) perforatum (Hypericum is wort a medici - on various cancer types have been have types cancer various on perforatum H. Mehtap KILIÇEREN 1Adnan Menderes University, Faculty ofMedicine,1DepartmentMedical Biology, 3 DepartmentofMedical Biochemistry, 09100Aytepe Campus,Aydın, Türkiye PERFORATUM PERFORATUM otis nme of number a contains perforatum H. International Symposium onDrugResearch &Development 2011 1 , Özlem ÖZ 2Department ofMedical Pharmacology, ON PEDIATRIC SARCOMA CELLS SARCOMA PEDIATRIC ON *[email protected] 2,* , Leyla DidemKOZACI DRD 2011 P-093 148 - - - 2. tidyl transferase-mediated dUDP nick-end labeling)assay.tidyl transferase-mediated dUDPnick-end deoxynucleo (terminal TUNEL by measured was Apoptosis test. release dehydrogenase) (lactate LDH the with sessed as- was cytotoxicity while WST-1, assay tetrazolium-based the using measured was activity metabolic proliferation/ andp53deficient,respectively2. wild type (rhabdomyosarcoma) and A673 (Ewing’s sarcoma), which are A204 as such lines cell sarcoma pediatric of growth the on of effects inhibitory lyzethe strategies inRMSandES. treatment future of development the for utilized be might suggest after incubation with IC50 dose of tested been have that lines cell both in shown was toxocity µg/ml. 50±16 of value IC50 with line cell A673 on effect inhibitory tory concentrations) of 10±2,5 µg/ml. Whereas it showed less inhibi- (half-maximal value IC50 with cells A204 of growth manner. dependent dose and time a in cells A673 and A204 both on cytotoxicity showed Kılıç M, Kasperczyk H, Fulda S, Debatin K-M. Role of hy of Role K-M. Debatin S, Fulda H, Kasperczyk M, Kılıç sistance. Oncogene 26(14):2027-2038,2007. re apoptosis of modulation in factor-1a inducible poxia ee w rpr fr h frt ie that time first the for report we Here, Cell test. blue trypan by determined was viability Cell ppoi, s n nelig ehns o ti cy this of mechanism underlying an as Apoptosis, as a potential anticancer agent which agentanticancer potential a as perforatum H. 3 , Mustafa BİRİNCİOĞLU L. extract extract L. perforatum Hypericum HYPERICUM HYPERICUM niie the inhibited perforatum H. . H. perforatum Our results

perforatum H. 2 - - - - POSTER PRESENTATIONS ------in-vitro 2003. - 2 )-pyrazole )-pyrazole deriva H This This study was supported by the Acknowledgment * Novel 3,3a,4,5,6,7-hexahydroindazole Novel 3,3a,4,5,6,7-hexahydroindazole Pharm Med Chem 336: 551-559, 336: Chem Med Pharm Gülberk UÇAR , Gülberk Hacettepe Hacettepe University Research Fund Number: 010D03301003). (Project 1, * H-NMR, mass and elementary analysis. In order to to order In analysis. elementary and mass H-NMR, 1 Arch Pharm Arch . All the synthesized compounds were investigated . All were investigated compounds the synthesized 9 Therefore, it Therefore, is tempting to develop new MAO inhibitor Güven Güven K. Synthesis and antimicrobial activity of some thiazolyl-pyrazoline derivatives. Phosphorus, Sulfur, Sili- Relat Elem 182: 749-764, 2007. con and arylthiazolylpyrazoline derivatives as anti-inflammatory anti-inflammatory as derivatives arylthiazolylpyrazoline and agents. A novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer’s disease. Med Chem 15: 2601-2610, 2007. Bioorg Syntheses and structural characterization of 1-(4-phe nyl-2-thiazolyl)-3-(4-methylphenyl)-5-(2-furyl)-4,5-di and 1-(4-(4-fluoro)phenyl-2-thiazolyl)- hydro-(1H)-pyrazole 3-(4-methylphenyl)-5-(2-furyl)-4,5-dihydro-(1H)-pyrazole. 2010. 700-705, 29(5): Chem Struct J Chinese Kaplancıklı ZA, Turan-Zitouni G, Özdemir A, Revial G, Nasr MNA, Said SA. Shiradkar MR, Akula KC, et al. Clubbed thiazoles by MAOS: MAOS: by thiazoles Clubbed al. et KC, Akula MR, Shiradkar Şahin ZS, Işık Ş, Salgın-Gökşen U, Gökhan-Kelekçi N.

agents, a hybrid molecules containing both pyrazole and thia and pyrazole both containing molecules a hybrid agents, 1-[4-(4-Substituted)phenyl-2-thiazolyl]-3-(4-sub zole moieties. stituted)phenyl-5-(2-furyl)-4,5-dihydro-(1 novel the afford to bromides phenacyl using cyclized were tives indi were compounds the of structures The pyrazolothiazoles. IR, by cated dertaken by MAO isoforms inhibit for to their ability selectively MAO-B liver rat inhibit to found were compounds the All tests. manner. competitive a in reversibly and selectively obtain information about the stereochemistry of the molecules molecules the of stereochemistry the about information obtain un were analyses X-ray structure, assigned the confirm to and 6. 7. 8. 9. - - - - - 149 P-094 DRD 2011 DRD [email protected] Nesrin GÖKHAN KELEKÇİ , Nesrin * Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, University, Hacettepe of Pharmacy, Faculty Department of Biochemistry, 1 2 Türkiye Ankara, 06100 Sıhhiye, PYRAZOLOTHIAZOLES DERİVATİVES International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Umut SALGIN GÖKŞEN Umut SALGIN

, e.g. antibacterial, antifungal, antiinflamatory, - an yrazolines yrazolines are well known and important nitro gen containing five membered heterocyclic - com pounds. Several pyrazoline derivatives have been

MONOAMINE OXIDASE INHIBITORY EFFECT SYNTHESIZED OF NEWLY by by the reaction of chlorochalcones Arkivoc IX: 344-352, 2005. with hydrazines. REFERENCES therapeutic approach in Alzheimer disease: Some novel pyr novel Some disease: Alzheimer in approach therapeutic investigation 2000. and preliminary 635-641, derivatives 35: Chem Med J thiazolyl-pyrazoline Eur activity. hypotensive their of tial antibacterial and antifungal agents. Indian J Sci Indian Pharm agents. and antifungal antibacterial tial 2008. 102-105, 70: antiinflamma and inhibitors MAO-B dual as derivatives azole 2007. 5775-5786, 15: Chem Med Bioorg analgesics. tory sis and antituberculous activity of - fluorinated 3-R-hydra zino-2-benzoylacrylates and their cyclization products. Chem J 36: 585-587, 2002. Pharm On the other hand, the nitrogen and sulfur heterocyclic Kini S, Gandhi AM. Novel 2-pyrazoline derivatives as poten as derivatives 2-pyrazoline Novel AM. Gandhi S, Kini Levai Levai A. Synthesis of chlorinated 3,5-diaryl-2-pyrazolines Nosova Nosova EV, Kravchenko MA, Lipunova GN, et al. Synthe Gökhan-Kelekçi N, Yabanoğlu S, Küpeli E, Salgın U, et al. A new new A al. et U, Salgın E, Küpeli S, Yabanoğlu N, Gökhan-Kelekçi some of Synthesis K. Erol FS, Kiliç P, Chevallet G, Turan-Zitounia P

Department of Pharmaceutical Chemistry, Chemistry, Department of Pharmaceutical 1 2. 1. 5. 3. 4. systems systems are very interesting because of their - physicochemi and drugs new of design the to relevance with properties cal new materials. In that respect, compounds containing the thiazole ring system are known to possess - pharmacologi cal properties such as tuberculostatic, antimicrobial, - antiin flamatory, analgesic and antibacterial activities5-7. Literature survey reveals 2-aminothiazole derivatives as the potential inhibitors of cdk5/p25 for the treatment of Alzheimer’s dis- 8. disorders ease and other neurodegenerative found found to possess considerable biological activities which stimulated research activities in this field1. Their prominent effects are activities2-4. and antidepressant hypotensive algesic, POSTER PRESENTATIONS 1. ay GNP nmtds f ml rmnns n ri sur roundings, ofIran. northwest Urmia in ruminants small of nematodes (GIN/P) nary Triclabendazole/ml)mg 50 evaluate the effects of effects the evaluate to conducted was study present The populations2. parasitic areas’ different in resistance AH minimize to doses ficient ef- in combination new formulate to necessary is it ment, develop constant a shown has resistance AH of nomenon phe the considering However, parasites. these for control of cornerstone the represented have drugs (AH) thelmintic an - ago; decades some nematodes1.From particularly sites, para- pulmonary gastrointestinal/ is countries developing the in ruminants small of production to constraint main the hn 0 ntrly evl ifce sheep infected heavily naturally 100 then technique3 Baerman and master Mc using count larva egg/ faecal sexes aged above 4 month were to subjected primarily PREVALENT GASTROINTESTINAL/PULMONARY NEMATODES OF SMALL SMALL OF NEMATODES GASTROINTESTINAL/PULMONARY PREVALENT S Max RA. Effect of repeated wattle tannin drenches tannin wattle repeated of Effect RA. Max REFERENCES One thousand free grazing sheep and goats of both 143, 2010. goats. and Vet138- Parasitologysheep 169: in tions infec nematode acquired naturally during ability on worm burdens, faecal egg counts and egg hatch- EVALUATION OF A NEW ANTHELMENTIC COMBINATION EFFICACY ON ON EFFICACY COMBINATION ANTHELMENTIC NEW A EVALUATIONOF 1 Department ofPathobiology, Faculty ofVeterinary Medicine,Shabestar Branch, IslamicAzadUniversity ,Shabestar, Iran 2 Department ofPathobiology, Faculty ofVeterinary Medicine,UrmiaBranch, IslamicAzadUniversity ,Urmia,Iran aiis n ot eeoig onre. However, countries. developing most in families resource-poor many of income and security food to contribution significant a make ruminants mall Felonil International Symposium onDrugResearch &Development 2011 against gastrointestinal/ pulmo gastrointestinal/ against ®

(37.5 mg Levamisole HCl and HCl Levamisole mg (37.5 Mohammad SADAGHIAN RUMINANTS IN URMIA, IRAN IRAN URMIA, IN RUMINANTS * [email protected] DRD 2011 P-095 150 - - - - - 2. 3. administration AH resistance rule. economicallimportant nematodes avoiddose lowand essaryto elevate the dose to cover 100% efficacy against todeswhereas about97%nematodesGIN nec isitand nema pulmonary against efficacy 100%company, has ministrationofthe dose recommended by manufacturer tothe end of study (P<0/05). Theresults showed that ad crease in EPG/ LPG levels of different sampling sessionswas observed up from first day and there was significant de ropsied to investigate GIN/Pnematodes. the end of period, 5 animals from each at group were nec Also, techniques. mentioned using examined was (EPG/LPG) faeces of gram per egg/larva subjects. Nematodes group each from post-treatment day and 14th 7th 3rd, 1st, at rectum from directly taken were samples Faecal placebo. as saline normal of amounts 1ml/5 kg BW of drenched were A group Then groups. equal two into and goats were selected for the study and were divided 1,* orsAot JJ ad ot H Atraie r im- or Alternative H. Hoste and JFJ.Torres-Acosta ruat M ad tes Vtrnr Parasitology. Veterinary others. and GM. Urquhart p. 276-281. Research 77:159-173,2008. Ruminants Small goats. and sheep grazing in ism parasit gastro-intestinal limit to methods proved 2 nd The effect of treatment on GIN/ P nematodes EPG/ LPG , Sohrab RASOULI ed., United Kingdom: Blackwell Publishing, 2003,

Felonil ®

whereas group B received equal 2 ------POSTER PRESENTATIONS - - - - -

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val DAD1 A, Sig=280,4 Ref=360,100 (TEST\17031100.D)Ref=360,100 Sig=280,4 A, DAD1 0 bles and fruits as an inhibitor of 8-hydroxydeoxy guanosine formation in vitro and in a rat 38(5): carcino Toxicology Chemical and Food model. genesis 467-471, 2000. fluence fluence of phenolic compounds from wines on the growth of Listeria monocytogenes. Food Control 18(5): 587-593, 2007. turkii and their in vivo anti-inflammatory and - anti nociceptive activities. Journal of - Ethnopharmacol ogy 112(2): 356-360, 2007. The The optimized chromatographic method was care Kasai H, et al. Action of chlorogenic acid in - vegeta Küpeli Küpeli E, et al. Phenolic compounds of Vaquero MJR, Alberto MR, Manca de Nadra MC. In-

0 80 60 40 20 100 mAU 6. 4. 5. perature. perature. 5mM KH (Figure 1) (Figure set at 215, 254, 280 and 323 nm. The resolution values set at 215, 254, 280 values and 323 The nm. resolution 1.5. than higher were acids phenolic of separation for 1. Figure of chromatogram HPLC phenolic acids at 280 nm. Consequent and accuracy. precision for fully validated ly, the described method will be employed to deter in fruit juices. mine phenolic compounds phosphoric phosphoric acid. Analysis was run at a flow rate of 1 mL.min - - - - and

151 P-096 DRD 2011 DRD phenolıc

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Tuğba İDUĞ, Ebru BÜYÜKTUNCEL Tuğba solution (pH 3.5) - solution ace 4 4 development

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İnönü University, Faculty of Pharmacy, Department of Analytical Chemistry, 44280 Malatya, Türkiye Türkiye Malatya, 44280 Chemistry, Department of Analytical of Pharmacy, Faculty İnönü University, henolic acids are widely distrubuted in the plant kingdom and are present in, e.g. tea, fruits, red beverages wine, and various medicinal 1. plants

HPLC M different different for your health? Cardiovascular Research 73(2): 341-347, 2007. liquid-liquid microextraction and high-performance and microextraction liquid-liquid liquid chromatography-diode array detection for the determination of phenolic acids in fruit juices. Chemistry 123(4): 1310-1317, 2010. Food fruit juices by isocratic column liquid - chromatogra Journalphy. of Chromatography A 891(1): 183-188, 2000. REFERENCES The separation was achieved on a with was achieved C18 column The separation A reversed-phase high performance liquid chromato Halliwell Halliwell B. Dietary polyphenols: Good, bad, or in- Saraji M, Mousavi F. Use of hollow fibre-based liquid- fibre-based hollow of Use F. Mousavi M, Saraji

Amakura Y, et al. Determination of phenolic acids in Y, Amakura P 3. 2. 1. a mobile phase a of phase 5 mobile mM KH tonitrile tonitrile (92:8) under at isocratic conditions room tem . They They are bioactivebenzoic acids2. compounds participate in diary diet and They influence - are antitu antioxidant, health. phenolic antimutagenic, and antibacterial3-5. mor, Moreover, acids can inhibit DNA damage6. graphic method was improved for simultaneous - determi nation of phenolic acids (gallic acid, 3,4-dihydroxy benzoic acid, p-hydroxy benzoic acid, chlorogenic acid, vanillic acid, caffeic acid, syringic acid, p-coumaric acid and ferulic acid) in fruit juices. 2,5-dihydroxy benzaldehyde was used as an standard. internal Phenolic Phenolic acids include hydroxycinnamic acids and hydroxy POSTER PRESENTATIONS ticles is a prerequisite for drug delivery to a specific target nanoparticles preparationforthe used of was technology reactor MicroJet method novel a study this In limits. specified within tions - distribu size narrow yielding methods efficient and simple Production of forsuch nanoparticles drug targeting requires PC/eoirt nnprils FN ad HPMCP/Chito and (FHN)HPMCP/Fenofibrate nanoparticles stabilizer, as 407 poloxamer with (FN) nanoparticlesfibrate feno including prepared were formulations different Three differentnanoparticleprofilesfenofibrate.formulationsof of permeabilitycaco-2mucoadhesivenessprofiles,in-vitro and 2. 1. CHARACTERIZATION OF FENOFIBRATE NANOPARTICLES FOR ORAL DRUG DRUG ORAL FOR NANOPARTICLES FENOFIBRATE OF CHARACTERIZATION 2 Johannes Gutenberg University, Faculty ofPharmacy, Dept.ofBiopharmaceutics andPharmaceutical Technology 55099Mainz, P eik-iesde EM ad .. iesde Drug Liversidge. G.G. and E.M. Merisko-Liversidge, poor of causes the and properties Drug-like CA. Lipinski h ojcie f h suy a t cmae dissolution compare to was study the of objective The pounds. Toxicologic Pathology 36(1):43-48,2008. com- water-soluble poorly Formulating nanoparticles: logical and Toxicological 44(1):235-249,2000. Methods Pharmaco of Journal permeability. poor and solubility REFERENCES ological conditions. Thus, the use of classified par classified of use the conditions.Thus, ological physiin - nanoparticles of bio-distribution and iour article size is the parameter that determines behav [4] . Emre TÜRELİ International Symposium onDrugResearch &Development 2011 1 MJR PharmJetGmbH,66424Homburg, Germany 1,2,* , BerndBAUMSTÜMMLER * [email protected] DELIVERY DRD 2011 P-097 [1-2] Germany 152 - - - - - . 3. higher than the other nanoparticle formulations. significantly was FHCN for absorbed fenofibrate of amount was also reflected to the Caco-2 permeation studies where the potential.This ZETA positive and content chitosan high the formulationthat was attached to mucin was the FHCN due to Accordingtothein-vitro mucoadhesiveness studies, theonly fessif.in higher timesapproximately wasreleased4 amount lutionprofiles whereasfenofibratecase theofin powder, the significantdissofassifdifferenceno andfessifbetween was bufferused.Furthermore fornanoparticle formulations there forevery formulation within first 10 minutes regardless of the completed was dissolution nanoparticles, from fenofibrate of releasetheformulation slowed FHCN inchitosan of ence lutionmedia such asSIF, SGF, Fessif, Fassif. Although the pres nanoparticleformulationsdifferentcompareddissowerein san/FenofibratenanoparticlesDissolution(FHCN).profilesof Türeli AE, Penth B, Langguth P, Baumstümmler B, inven- B, P,Baumstümmler Langguth B, Penth AE, Türeli DE2010/075015 2010Feb. 11 PCT/ reactors. microjet in particles said coating for and particles refined highly pharmaceutically producing for method and Device assignee. GmbH PharmJet MJR tors; 1 ,

Peter LANGGUTH 2 - - - POSTER PRESENTATIONS - - , 3 c1-c7 being c13 being mixed- c5-7 c3, Barij N. SINHA , Barij N. 3 were were highly selective towards Bu- c12-17 being mixed-type reversible and reversible mixed-type being c14-17 1,* c12, diseases. Neurosci Lett 382(3): 327-31, 2005. Lett Neurosci diseases. mycobactin analogues as MAO-inhibitors. Bioorg Med 18(24): 6362-68, 2008. Chem Lett new and rapid colorimetric determination of acetylcho linesterase activity. Biochem Pharmacol 7(2): 88-95, 1961. 88-95, 7(2): Pharmacol Biochem activity. linesterase Jayaprakash V, Sinha BN, Ucar G, Ercan A. Pyrazolinebased Pyrazolinebased A. Ercan G, Ucar BN, Sinha V, Jayaprakash RM. A Featherstone V, Ellman GL, CourtneyAndres Jr. KD, Venkatesan JAYAPRAKASH , Venkatesan 3. 4. inhibit human AChE and BuChE using spectropho Ellman’s and AChE inhibited the compounds [4]. All method tometric BuChE at nM to low μM concentration. Compounds type reversible and the rest being non-competitive - irrevers ible. Compounds ChE, irreversible. noncompetitive were were highly selective towards AChE, 2 - - - 153 P-098 DRD 2011 DRD Gülberk UÇAR [email protected] * MAO/CHOLINESTERASE Bercis İmge UÇAR İmge , Bercis 1 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International , in the present work the acetylcholine es- Başkent University, Faculty of Medicine, 16. Sok No:11, Bahçelievler, Ankara, Türkiye Ankara, 16. Sok No:11, Bahçelievler, of Medicine, Faculty University, Başkent 2 1,2 Hacettepe University, Faculty of Pharmacy, Dept. of Biochemistry, 06100 Ankara, Türkiye 06100 Ankara, Dept. of Biochemistry, of Pharmacy, Faculty University, Hacettepe 1 Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, 835215, India 835215, Mesra, of Technology, Birla Institute Sciences, Department of Pharmaceutical 3

ince design strategy and advantages of dual inhibi- dual of advantages and strategy design ince tors in neurodegenerative disorders have been re viewed

thiocarbamoyl-3-phenyl-5-thienyl-2-pyrazolines: thiocarbamoyl-3-phenyl-5-thienyl-2-pyrazolines: a novel cholinesterase and selective monoamine oxidase B inhibitors for the treatment and of Alzheimer’s Parkinson’s ed ligands to combat neurodegenerative diseases. J MedJ diseases. neurodegenerative combat to ligands ed Chem 51(3): 347-72, 2008. V,Recanatini V,Recanatini M, Melchiorre C. (2008) Multi-target-direct REFERENCES Uçar G, Gökhan A, N, Yeşilada Bilgin AA. 1-N-Substituted

Cavalli Cavalli A, Bolognesi ML, Minarini A, Rosini M, Tumiatti S Samiye YABANOĞLU ÇİFTÇİ YABANOĞLU Samiye PYRAZOLINE-BASED MYCOBACTIN ANALOGUES AS DUAL INHIBITORS OF terase terase (AChE) and butrylcholine esterase (BuChE) inhibitory activities of the thirty two 3,5-diaryl-2-pyrazoline-1-thiocar bamoyl bamoyl derivatives which were synthesized as analogues of Mycobactin and evaluated as potent MAO 3 inhibitors were determined. Each compound was evaluated for its ability to 2. 1. POSTER PRESENTATIONS fects of nitrite of fects ef- protective possible the investigate to was study present n prxds, ueoie imts, aaae wr de were catalase) dismutase, superoxide peroxidase, one glutathi- reductase, glutathione (glutathione-S-transferase, activities antioxidantlevels,(GSSG)glutathioneand enzyme group. Malondialdehyde (MDA), reduced (GSH) and oxidized were found to be increased in I/R group compared to control quantitative indices of liver damage. These activities enzyme dehydrogenase were activities determined as (LDH) enzyme lactate and (AST) aminotransferase aspartate and (ALT)rase aminotransfe alanine Serum protocol. I/R to prior hours 24 and 12 given nitrite sodium of µg/kg) 1650 165, 16.5, (1.65, concentrations different 4 with administrated groups study and reperfusion) hours 5 and ischemia minutes protocol(45 Groupswere control,miceas 6 consist of arranged I/R sham, collected. were samples tissue and blood mice, g 25-30 and mia and 5 hours reperfusion period performed on 8-10 week model. I/R hepatic mouse in I/R ring du- activated processes inflammatory the on periods time Bercis İmgeUÇAR H INFLAMMATORY PROCESSES ACTIVATED DURING HEPATIC ACTIVATED ISCHEMIA- DURING PROCESSES INFLAMMATORY INVESTIGATION OF THE PROTECTIVE EFFECT OF SODIUM NITRITE ON ON NITRITE SODIUM OF EFFECT PROTECTIVE THE OF INVESTIGATION n n rscinl ugr.Te ups o the of purpose The surgery. resectional and on transplantati- liver with associated complication major a is injury (I/R) ischemia-reperfusion epatic REPERFUSION (I/R) INJURY IN MOUSE HEPATIC MODEL I/R MOUSE IN INJURY (I/R) REPERFUSION

3 administrated in different concentrations and concentrationsdifferent in administrated Hacettepe University, Faculty ofPharmacy, Dept.ofPharmacology, 06100Ankara, Türkiye 2 Hacettepe University, Faculty ofPharmacy, Dept.ofBiochemistry, 06100Ankara, Türkiye 1 Başkent University, Faculty ofMedicine,16. SokNo:11,Bahçelievler, Ankara, Türkiye 1 , Açelya YALOVAÇ ASLAN International Symposium onDrugResearch &Development 2011 After 45 minutes ische minutes 45 After * [email protected] Gülberk UÇAR DRD 2011 P-099 2 154 , Samiye YABANOĞLU ÇİFTÇİ - - - these parameters inthesamestudygroups. all examining mice,and on performing of terms in unique is study injury.This I/R on effect protective significant have to found were administration nitrite findings, these on Based administration. before hours 12 to compared before hours 24 administred when effective more be to determined were nitrite of effect cytoprotective the Moreover, administered. nitrite of concentration the on depending levels control to ters determined to change with I/R protocol, were decreased parame all nitrite, sodium with administrated were which groups study all In group.control to compared group I/R in cytokines IL-1β,(TNF-α, IL-6, IL-8 proinflammatory and IL-12) were significantly increased of levels Plasma group. I/R in demonstrated that liver wasMPO activity markedly elevated leukocyte infiltration in liver tissue of study groups and it was of indicator the as measured was activity (MPO)peroxidase Myelo group. I/R in lowered significantly be to found were activities enzyme antioxidant All group. I/R the in increased significantly decreased; GSSG and MDA content significantly be to found were ratio GSH/GSSG and content GSH groups. study and sham control, of samples tissue liver in termined 2,* 2 , Bülent GÜMÜŞEL 3 , - - POSTER PRESENTATIONS - - - Cl , 2 value of 5.6 mM. 50 O Cl S 3 N H N N S N KUC100309 Neerja KAUSHİK-BASU , Neerja 1 Tanaji T. TALELE T. , Tanaji 2 Cl M. Eur J Med Chem 41, 353, 2006. M. Eur 13, 3857, 2008. in Bioscience ŞG. Frontiers Küçükgüzel Küçükgüzel Küçükgüzel ŞG, Güllüce Kocatepe A, De Clercq E, Şahin F, TT, Talele Y, Chen A, Basu A, Bopda-Waffo Kaushik-BasuN, analogues of these scaffold as HCV - eva NS5B We inhibitors. four identifed and scaffold this of derivatives eigtheen luated ac RdRp NS5B 50% than greater exhibited which derivatives tivity inhibition at 100 micromolar compound concetration. Further evaluation of their inhibitory activities resulted in the identification of 2-{[5-(4-chlorophenyl)-1,3,4-thiadiazol- 2-yl]imino}-5-(2,6-dichlorobenzylidene)-1,3-thiazolidin-4- one (KUC100309) which exhibited an IC Molecular docking of this derivative within the pockets of NS5B suggested its binding allosteric at the allosteric poc ket (AP)-2 on NS5B and provided clues towards further op timization and synthesis of new derivatives with improved anti-NS5B activity. In the light of modeling experiments of KUC100309, four new derivatives were then designed and synthesized in order to be evaluated as inhibitors of HCV Results will be discussed in detail. NS5B. 3. 4. Esra TATAR , Esra 1 - - - - Türkiye 155 P-100 DRD 2011 DRD 11439 York New POLYMERASE *[email protected] as novel HCV 2 and 5-arylidene 1 by Ş.G.Küçükgüzel 3 , İlkay KÜÇÜKGÜZEL 1,* International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Guru Kumar Kollongod RAMANATHAN Guru Kumar Kollongod . Here we report on the identification of novel novel of identification the on report we Here . 4

New Jersey Medical School, Department of Biochemistry & Molecular Biology, NJ 07103, USA. NJ Biology, & Molecular School, Department of Biochemistry Medical Jersey 2New hogen of global public health significance with an estimated prevalence of 200 million people epatitis epatitis C virus (HCV) is an important human pat Gökhan SATILMIŞ Gökhan

5-ARYLIDENE-4-THIAZOLIDINONES AS INHIBITORS OF HCV NS5B eu M, Kaushik-Basu N. Bioorg Medeu M, Kaushik-Basu Chem 18, 4630, 2010. N. Bioorg 18, 6114, 2008. Med Chem Lett REFERENCES Talele TT, Arora P, Kulkarni SS, MR, Patel Singh S, TT, Arora P, Chuday Talele Rawal RK, Katti SB, Kaushik-Basu N, Arora P, Pan Z. Rawal Pan Bioorg RK, Katti SB, Kaushik-Basu N, P, Arora H Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, İstanbul, Haydarpaşa 34668 Chemistry, of Pharmaceutical Department of Pharmacy, Faculty University, 1Marmara St. John’s University, Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, Health Professions, of Pharmacy and Allied College Sciences, Department of Pharmaceutical University, 3St. John’s 2. 1. world-wide and a predicted 100,000 new-cases each year. Per year. each new-cases 100,000 predicted a and world-wide sistent sistent HCV infection is the leading cause of hepatitis severe - hepatocellu and steatosis, cirrhosis, to progresses often that current and HCV against vaccines no are There carcinoma. lar therapeutic options are limited in efficacy against various HCV genotypes and in addition are associated with draw backs of specificity Therefore and the toxicity. development priority. high of area an is HCV against agents antiviral new of HCV NS5B RNA-dependent RNA polymerase is a viral pivotal with no functionalprotein genome in replicating equivalent the host and therefore represents an attractive therapeutic target. Previously, we had reported on the identification of 2-Aryl-3-heteroaryl-1,3-thiazolidin-4-ones NS5B inhibitors. N-[2-(2-fluorophenyl)-4-oxo- 2’,4’-Difluoro- 1,3-thiazolidin-3-yl]-4-hydroxybiphenyl-3-carboxamide, which was designed and synthesized derivatives derivatives of 4-oxo-2-thionothiazolidines et.al., et.al., have been reported to inhibit NS5B polymerase non- competetively POSTER PRESENTATIONS evaluation were determined by to show antifungal activity. antimicrobial their and synthesized been have derivatives ester oxime etanon H-pyrazol-1-yl)1-(naphtalene-2-yl)-2-(1 new two study this in Therefore, mg/ml)2. (12.5 centration con- low at activity antifungal showed compounds these of most that found and derivatives ether oxime pyrazol-1-yl) antineoplastic therapy1. or corticosteroid prolong as such conditions compromise immune and transplants organ AIDS, have who patients the for needed are agents antifungal better new of synthesis reasons, these For drugs. antifungal current of effects side and infections fungal resistant the of because mandatory sis of new systemic antifungal medications has been getting synthe The drugs. antifungal of family expanding rapidly a 2. 1.

A ÖzdemirZ. P.Sapra S, Dis- Rastogiand R, VenkataramananM, Kidwai H- 1-(2-naphtyl)-2-(1 new some prepared we Previously, Üniversitesi, Sağlık Bilimleri, Yüksek lisans Tezi, Malatya. tezleri,antikonvülsanantimikrobiyalve aktiviteleri, İnönü ınfective agents, Curr Chem2:27-71,2003. Med anti- compounds antifungal of development and covery REFERENCES 3İnönü University, Faculty ofPharmacy, DepartmentofPharmaceutical Microbiology, 44280Malatya, Türkiye 2İnönü University, Faculty ofPharmacyDepartmentPharmaceutical Chemistry, 44280Malatya, Türkiye SYNTHESIS OF NEW PYRAZOLE DERIVATIVES AS ANTIMICROBIAL ANTIMICROBIAL AS DERIVATIVES PYRAZOLE NEW OF SYNTHESIS practice forpractice a long time. The azole antifungals are clinical in using been have and drugs infective anti- of part important an are agents ntifungal Yeni(arilalkil)pirazol türevi oksim eterlerin sen 1Undergraduate student ofİnönüUniversity, Faculty ofPharmacy, 44280Malatya, Türkiye International Symposium onDrugResearch &Development 2011 Bünyamin ŞIK *[email protected] 1 , ArzuKARAKURT AGENTS DRD 2011 P-101 156 - - lis, pounds was confirmed by IR, comof structure the and below given is scheme synthesis 4. 3. undergraduate student. 3,4. ods for andantifungal activities antibacterial and cans microorganisms: N H lncl n Lbrtr Sadrs nttt, Approved Institute, Standards Laboratory and Clinical Approved Institute, Standards Laboratory and Clinical h cmons ae en rprd codn t the to according prepared been have compounds The tnadScn Eiin NCS ouet M27-A2, Pennsylvania, 2002. document NCCLS Edition. Standard-Second sylvania, 2003. Penn- M7-A7, Document CLSI Edition, Standard-Seventh Acknowledgement: following the against evaluated were compounds The shrci coli , Escherichia 2 O H

H 2,* O C l by using modified agar dilution meth - dilution agar modified using by tropicalis C. , SelamiGÜNAL B r 2 Staphylococcus aureus, Staphylococcus N suooa aeruginosa, Pseudomonas O H N N This study is a part of final project of O 1 H-NMR and Mass spectral data. 3 Br ( C H 3 C H H N 2 C N a N N H O 2 C C 2 O O C ) l 2 O Enterococcus faeca- Enterococcus add albi- Candida O O N O O N O N 2 O N N N N N N POSTER PRESENTATIONS 3 - 3 3 H H H C 2 C C 5 4 3 3 H ) ) 2 H H C 2 C C C H H C C N N ( ( - -

= N R Staphy O 3 N N R O Escherichia , coli N N N N H F Br M D a

Selami GÜNAL , Selami /

N X O R 2,* N N H O Enterococcus Enterococcus , faecalis N 2 r B O H-NMR and Mass spectroscopic methods were l 1 C H

H , Arzu KARAKURT O IR, Standard-Seventh Standard-Seventh Edition, CLSI Document M7-A7, - Penn , 2003. sylvania Standard-Second Edition. NCCLS document 2002. Pennsylvania, M27-A2, Clinical and Laboratory Standards Institute, Approved Clinical and Laboratory Standards Institute, Approved 2 2 H N used for elicitation of their structure. Evaluation of their of Evaluation structure. their of elicitation for used antibacterial and antifungal activities was realised by using modified agar dilution methods against lococcus , aureus - and C. tropi albicans Candida aeruginosa Pseudomonas 3,4. calis 3. 4. - 157 P-102 DRD 2011 DRD [email protected] * Mehmet Abdullah ALAGÖZ , Mehmet 1 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Faculty of Pharmacy, Department of Pharmaceutical Microbiology, 44280 Malatya, Türkiye 44280 Malatya, Microbiology, Department of Pharmaceutical of Pharmacy, Faculty

Undergraduate student of İnönü University, Faculty of Pharmacy, 44280 Malatya, Türkiye 44280 Malatya, of Pharmacy, Faculty of İnönü University, student Undergraduate 1

Fatime BEYTÜT Fatime

İnönü University, Faculty of Pharmacy Department of Pharmaceutical Chemistry, 44280 Malatya, Türkiye 44280 Malatya, Chemistry, of Pharmaceutical of Pharmacy Department Faculty İnönü University, 2 STUDIES ON THE NEW OXIME ETHERS OF 1-(2-NAPHTYL)-2-(1,2,4- TRIAZOL-1-YL)ETHANONE AND THEIR ANTIMICROBIAL ACTIVITIES İnönü University, n the past decades, incidence of antimicrobial - resis world the in increased has infections microbial in tance - cancer and trans organ with patient HIV, especially for 3 These These compounds have been synthesized starting Azole antifungals are important for the treatment of treatment the for important are antifungals Azole Özbey S, Dalkara S. Synthesis of some oxime ether deriva- ether oxime some of Synthesis S. Dalkara S, Özbey tives of 1-(2-naphthyl)-2-(1,2,4-triazol-1-yl)ethanone and their anticonvulsant and antimicrobial activities. Arch 339: 513-520. 2006. Pharm Ther 8(6): 639-41, 2010. Ther REFERENCES Karakurt A, Aytemir Özalp MD, Stables M, JP, Kaynak, FB, Razonable RR. Antifungal Therapy. Razonable Expert RR. Therapy. RevAntifungal Anti Infect I from 2-acetylnaphthalene as given below: as given 2-acetylnaphthalene from invasive fungal infections which have a growing impor growing a have which infections fungal invasive ether oxime new three prepared we study this In tance. derivatives with triazole ring as a continuation of our 2. derivatives in azole interest 2. 1. plantation. For this reason development of new and more ef- more and new of development reason this For plantation. fective antimicrobial agents are urgent needs for treatment infections1. of resistance POSTER PRESENTATIONS gns ih etr ciiy rfl i a atatv ae for medicinal chemists. area attractive an is profile activity better with agents antifungal new of development Therefore recurrence1. of probability the in increase the to due agents antifungal tive 2. 1. most of the these compounds showed antimicrobial ac (1,2,4-triazol-1-yl)oxime ether derivatives and found that their structure. in ring triazole has which market the in drugs tifungal an- rhe of examples the are terconazole itraconazole, Fluconazole,derivatives. azole other the among tance impor special a havetherapy. derivativesTriazoleoral treatment of immune compromised patients who need F Karakurt A, Aytemir MD, Stables JP, Özalp M, Kaynak, FB, Kaynak, JP,M, Stables MD,Özalp Aytemir A, Karakurt teda- enfeksiyonlarının mantar Sistemik M. Alp C, Kuş hi atcnusn ad niirba atvte. Arch activities. antimicrobial and anticonvulsant their and 1-(2-naphthyl)-2-(1,2,4-triazol-1-yl)ethanone of tives Özbey S, Dalkara S. Synthesis of some oxime ether deriva- Derg 31(2):91-131,2002. Fak Ecz Ankara bileşikler. yeni ve hedefler yeni visinde REFERENCES rvosy w peae sm nw 1-(2-naphtyl)-2- new some prepared Previously, we the in role key a maintained have antifungals Azole 3 SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL OXIME OXIME NOVEL SOME OF ACTIVITY ANTIMICROBIAL AND SYNTHESIS İnönü University, 2 İnönü University, ETHER DERIVATIVES OF 1-(2-NAPHTYL)-2-(1,2,4-TRIAZOL-1-YL) OF DERIVATIVES ETHER essary to treat these them with systemically effec systemically with them these treat to essary compromised patients than the others and it is nec immune in seriously more occur infections ungal Nagihan KAYA 1 Undergraduate student ofİnönüUniversity, Faculty ofPharmacy, 44280Malatya, Türkiye

Faculty ofPharmacy, DepartmentofPharmaceutical Microbiology, 44280Malatya, Türkiye

Faculty ofPharmacy, DepartmentofPharmaceutical Chemistry, 44280Malatya, Türkiye International Symposium onDrugResearch &Development 2011 1 , MehmetAbdullahALAGÖZ * [email protected] ETHANONE DRD 2011 P-103 158 - - - - albicans aeruginosa,Escherichia coli reus poundshasbeen tested agains com two(+)Gr( the of Antimicrobial activity data. spectral Mass and 4. 3. their synthesis scheme are given below. bacterialactivities. Thestructure of the compounds and antifungal/antievaluatetheirto and triazolering with derivativesoximeetherdesignnew to aimed we study tivitity at low concentration (16 N H 2 2 , ArzuKARAKURT O lncl n Lbrtr Sadrs nttt, Approved Institute, Standards Laboratory and Clinical Approved Institute, Standards Laboratory and Clinical tnadScn Eiin NCS ouet M27-A2, Pennsylvania, 2002. document NCCLS Edition. Standard-Second sylvania, 2003. Penn- M7-A7, Document CLSI Edition, Standard-Seventh Pharm 339:513-520.2006. Theirstructures ofthehave been confirmed byIR, , H Enterococcus faecalis

H C l , O C. tropicalis B r 2 N O H ) by modified agar dilution method N N ) and two Gr (-) bacteria ( ) andtwoyeasts) likefungi ( R O 2,* X N

a A , SelamiGÜNAL c Br e t o ne H N N m g/ml) N N 2 O . Therefore in this Staphylococcusau R N N O Pseudomonas R 3 = N N N C C C C H H H H Candida 1 3,4 2 C 2 3 C H-NMR C H H H 2 . 2 C 2 C C H H H 3 2 C H C H 3 2 - - - POSTER PRESENTATIONS - , 4 2.1390 Quantitation Quantitation limit (μg/mL) Nurullah ŞANLI , Nurullah 3 0.6417 Detection limit (μg/mL) coeff. Correl. Correl. 0.9995 SE of 5 0.025 intercept Guideline. Under the given chromatographic conditions, AML and ICH Steering Committee (2005). Harmonized Tripartite Mustafa Sinan KAYNAK Sinan , Mustafa 2. tion volume was 20 µL and total run time for an assay was approximately 5 min. A loop diuretic furosemide (FSM) was used as the internal standard. The developed method was validated according to the ICH guideline [2]. For application of the proposed HPLC method, commercially available four different AML containing tablets (one reference and three generic tablets) were obtained from the market and analy their drug content. sed for FSM were eluted at 4.28 and 3.68 The minutes, respectively. method was linear in the concentration range of 1.0 to 16.0 µg/mL, and limit of quantitation was 2.139 µg/mL (Table 1). Under the conditions used, the analysis completely fulfilled the system suitability test limits suggested by FDA for the quantitative chromatographic methods. The method was successfully applied for the analysis of AML in commercially tablets. available 2,* - - SE of slope 0.003 159 P-104 DRD 2011 DRD Selma ŞAHİN [email protected] * -0.040 Intercept 0.176 Slope C during the analysis, was used was analysis, the during C column (Fortis™ 250x4.60 mm o Kamile Zümrüt DİRİCAN , Kamile 1 18 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International Linearity 1.0-16.0 n=6 range (μg/mL) range İnönü University, Faculty of Pharmacy, Undergraduate Student, 44280 Malatya, Türkiye 44280 Malatya, Student, Undergraduate of Pharmacy, Faculty İnönü University, Hitit University, Faculty of Science and Arts, Dept. of Chemistry, 19040 Çorum, Türkiye of Chemistry, and Arts, Dept. of Science Faculty Hitit University, 2 4

mlodipine (AML) (as besylate, mesylate or male ate) is a long-acting calcium channel blocker (di- hydropyridine) used as an anti-hypertensive and İnönü University, Faculty of Pharmacy, Dept. of Pharmaceutical Technology, 44280 Malatya, Türkiye 44280 Malatya, Technology, Dept. of Pharmaceutical of Pharmacy, Faculty İnönü University, 3 Süleyman Demirel University, Faculty of Science and Arts, Dept. of Chemistry, 32100 Isparta, Türkiye 32100 Isparta, and Arts, Dept. of Chemistry, of Science Faculty University, Demirel Süleyman 1 Hacettepe University, Faculty of Pharmacy, Dept. of Pharmaceutical Technology, 06100 Ankara, Türkiye 06100 Ankara, Technology, Dept. of Pharmaceutical of Pharmacy, Faculty University, Hacettepe

5 AML DEVELOPMENT OF RP-HPLC METHOD FOR THE DETERMINATION OF Fevziye Ö. ŞİMŞEK Fevziye AMLODIPINE IN COMMERCIALLY AVAILABLE DOSAGETABLET FORMS Stone LR, et al. Clinical Therapeutics 25: 35-57, 2003. Therapeutics Clinical LR, et al. Stone REFERENCES Statistical evaluation of the calibration data of the calibration evaluation 1. Statistical Table The The aim of this study was to develop a fast, new, reliable

Levine Levine CB, Fahrbach KR, Frame D, Connelly JE, Estok RP, A Compound 1. for for the separation and quantification of AML. The mobile phase consisted of water (15 mM o-phosphoric acid, pH 5.0) and acetonitrile (50:50 v/v). Analyses were run at a flow rate 1.0 mL/min and UV detector was set at 238 nm. The injec 5µm) which was heated at 45 at heated was which 5µm) and validated HPLC method for the determination of AML in tablet dosage forms. A C in the treatment of angina. AML actsof AML angina. the smooth in relaxing the by treatment muscle in the arterial wall, decreasing peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart muscle more [1]. than Currently, ten AML different (as besylate) containing tablets (5 and 10 mg) drug market. Turkish in the available commercially are POSTER PRESENTATIONS Na mmol/L 40 KCl, mmol/L 10 NaCl, mmol/L 25 containing tion solu- Golytely tubing. plastic with cannulated was cm) (10 jejunum the of segment a incision; longitudinal midline a by opened was rats the of abdomen Briefly, (n=7). method perfusion intestinal in-situ single-pass using rat the in gated asthereferencelected standard. se was drug, permeable highly a metoprolol, whereas (2), testinal membrane was used as the low marker permeability in- the across absorbed not is which red Phenol diclofenac, of permeability jejunal compare To preparation. perfusion situ-intestinal in pass single the in sodium diclofenac of ity - permeabil intestinal the investigate to designed was study This 1. side-effects serious other or ulcerations trointestinal NSAIDs, diclofenac iswell tolerated andrarely produces gas- 2. 1. n dcoea sdu (. m/L, eo 07 M phenol mM (0.7 zero mg/mL), (0.4 sodium diclofenac ing contain- medium perfusion The mL/min. 0.2 of rate flow a at medium perfusion this with intestinal perfused then was isolated segment The medium. perfusion the as chosen D 2 Milani PZ, Valizadeh H, Azarmi Y, Jalali MB, Tajerzadeh H. TajerzadehMB, Y, Azarmi Jalali H, PZ,Valizadeh Milani determina- chromatographic Liquid V. Kmetec R, Roškar eua preblt o dcoea sdu ws investi- was sodium diclofenac of permeability Jejunal and phenol red in samples from rat in situ intestinal per intestinal situ in rat from samples in red phenol and propranolol metoprolol, of determination Simultaneous B 788:57-64,2003 Chromatogr J fluid, synovial human in diclofenac of tion REFERENCES SO DETERMINATION OF PERMEABILITY OF DICLOFENAC SODIUM IN THE IN SODIUM DICLOFENAC OF PERMEABILITY OF DETERMINATION 4 2 mo/ NaHCO mmol/L 20 , 3 Hacettepe University, Faculty ofPharmacy, Dept.ofPharmaceutical Technology, 06100Ankara, Türkiye 1 Mustafa SinanKAYNAK İnönü University, Faculty ofPharmacy, Dept.ofPharmaceutical Technology, 44280Malatya, Türkiye n atprtc rpris Cmae t other to Compared properties. antipyretic and anti-inflammatory analgesic, with (NSAID) drug anti-inflammatory non-steroidal a is iclofenac 2 İnönü University, Faculty ofPharmacy, Dept.ofAnalytical Chemistry, 44280Malatya, Türkiye

IN-SITU INTESTINAL PERFUSION PREPARATION PERFUSION INTESTINAL IN-SITU International Symposium onDrugResearch &Development 2011 3 n 8 mo/ mnio was mannitol mmol/L 80 and 1 , Hatice ÇAĞLAR * [email protected] DRD 2011 P-105 160 - - 2,* using inlet (C inlet using werecalculated metoprolol tartarate and diclofenacsodium ability compound.ability perme high a as classified be can diclofenac results, our on compound.Based permeability high a consideredas is it lol, If a compound’s permeability is higher than that of metopro marker. permeability high the as used widely is Metoprolol .3 ± 0.19x10 (± 0.43 3. perfused intestinal segment. perfused (Q medium perfusion od developedod by Çağlaral. et Permeability [3]. values(P tubing and then analyzed with a reversed phase HPLC meth- outlet the from collected were samples perfusate intervals, time predetermined At min. 60 for perfused were markers red) and high (0.4 mg/mL metoprolol tartarate) permeability , EbruBÜYÜKTUNCEL Çağlar MS, S, Sahin BüyüktuncelH, Kaynak E. HPLC- Meth Sci 38(Suppl1):179-181,2009. Sci logical matrix for intestinal studies,perfusion Eur J Pharm bio in red phenol and metoprolol diclofenac, of nation determi- Simultaneous validation: and development od fusion studies, DARU 14(2):102-108,2006. P eff values estimated for metoprolol and diclofenac were diclofenac and metoprolol for estimated values P eff in = ) and outlet (C outlet and ) -4 ad .4 (±0.52x10 1.44 and ) ⎣ ⎢ ⎢ ⎡ − in Q , egh L ad imtr r o the of (r) diameter and (L) length ), in 2 . out 2 ln . , SelmaŞAHİN π ) concentrations, flow rate of rate flow concentrations, ) ⎝ ⎜ ⎜ ⎛ . r C . C l -4 out in c/, respectively. cm/s, ) ⎠ ⎟ ⎟ ⎞ l ⎦ ⎥ ⎥ ⎤ 3 eff

) of ) - - - POSTER PRESENTATIONS - - , 4 0.0311 Quantitation Quantitation limit (μg/mL) 0.0102 (μg/mL) Detection limit Nurullah ŞANLI , Nurullah 3 coeff. Correl Correl 0.9995 - cept 0.130 5 SE of inter Under the given chromatographic conditions, FSM and Guideline. ICH Steering Committee (2005). Harmonized Tripartite tion volume was 20 µL and total run time for an assay was approximately 5 min. A calcium channel blocker Amlodip ine (AML) was used as the internal standard. The proposed guideline2. ICH the to according validated was method HPLC For application of the method, commercially available two FSM different containing tablets and (one one reference ge neric tablet) were obtained from the market and analyzed their drug content. for AML were eluted at 3.68 and The 4.28 minutes, respectively. method was linear in the concentration range of 0.1 to 12.0 1). (Table µg/mL 0.0311 was quantitation of limit and µg/mL, Under the conditions used, the analysis completely fulfilled the system suitability test limits suggested by FDA for the quantitative chromatographic methods. The method was successfully applied for the analysis of FSM in commercially tablets. available 2. SE of - - - Mustafa Sinan KAYNAK Sinan , Mustafa slope 0.023 C o 161 2,* P-106 DRD 2011 DRD Selma ŞAHİN 0.052 [email protected] Intercept * 1.610 Slope Songül ERDOĞDU , Songül 1 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International column (Fortis™ 250x4.60 mm 5µm) (μg/mL) 18 0.1-12.0 n=7 Linearity range İnönü University, Faculty of Pharmacy, Undergraduate Student, 44280 Malatya, Türkiye Türkiye 44280 Malatya, Student, Undergraduate of Pharmacy, Faculty İnönü University, Hitit University, Faculty of Science and Arts, Dept. of Chemistry, 19040 Çorum, Türkiye of Chemistry, and Arts, Dept. of Science Faculty Hitit University, 2 4

İnönü University, Faculty of Pharmacy, Dept. of Pharmaceutical Technology, 44280 Malatya, Türkiye 44280 Malatya, Technology, Dept. of Pharmaceutical of Pharmacy, Faculty İnönü University, DEVELOPMENT AND OF VALIDATION A RP-HPLC METHOD FOR DETERMINATION OF FUROSEMIDE IN TABLET DOSAGE FORMS 3 Süleyman Demirel University, Faculty of Science and Arts, Dept. of Chemistry, 32100 Isparta, Türkiye 32100 Isparta, and Arts, Dept. of Chemistry, of Science Faculty University, Demirel Süleyman urosemide urosemide (FSM) is a loop diuretic commonly used in adults, infants and children for the treatment of edematous states associated with congestive heart 1 Fevziye Ö. ŞİMŞEK Fevziye Hacettepe University, Faculty of Pharmacy, Dept. of Pharmaceutical Technology, 06100 Ankara, Türkiye 06100 Ankara, Technology, Dept. of Pharmaceutical of Pharmacy, Faculty University, Hacettepe

5 FSM 319 (2000) 38-50. REFERENCES . Statistical evaluation of the calibration data of FSM by RP-HPLC of FSM by data of the calibration evaluation 1. Statistical Table The The aim of our study was to develop a fast, new, reliable Compound

D.C. D.C. Brater, Pharmacology of diuretics, Am. J. Med. Sci., F 1. ic acid) and acetonitrile (50:50 v/v). The pH of the phase mobile was adjusted to 5.0. The column was heated at 45 with a mobile phase consisted of water (15 mM o-phosphormM (15 water of consisted phase mobile a with during the analysis. Analyses were run at a flow rate 1 mL/ min and UV detection was performed at 238 nm. The injec and validated HPLC method the for and determination of HPLC validated FSM in tablet dosage forms. Chromatographic separation of FSM was achieved on a C mide may be used in adults for the treatment of hypertension alone or in combination with other antihypertensive 1. agents Currently, two different FSM containing tablets are drug market. Turkish in the available commercially failure, failure, cirrhosis of the liver and renal disease. Oral furose POSTER PRESENTATIONS from two commercially available Furosemide tablets. mg) (40 Furosemide of profiles release in-vitro the compare in the Turkish drug market. The objective of this study was to available commercially are tablets containing FSM different Currently,agentsantihypertensive3. other with bination two com- in or alone hypertension of treatment the for adults in used be may furosemide Oral disease. renal and liver the of tous states associated with congestive failure, heart cirrhosis edema- of treatment the for children and infants adults, in used commonly diuretic loop a is (FSM) Furosemide cess1,2. pro manufacturing the of scale-up the and manufacture, of those in the formulation, the manufacturing process, the site as such changes, certain after performance and quality duct pro the of sustainability the ensure and formulations; new developmentthe of guide product; drug controla of quality batch-to-batch the assess to used is capsules) tablets, (i.e. forms dosage oral solid release immediate for test solution dis- vitro in consideration, general this on Based formance. per vivo in of prediction the to relevant be may dissolution se of the critical nature of the first two of these steps, in vitro and the permeability across the gastrointestinal tract. - Becau conditions physiological under drug the of solubilization or 1. D Guidance for Industry: Dissolution testing of immediate of testing Dissolution Industry: for Guidance guidance/index.htm from Retrieved 1997. CDER, tion, Administra- Drug and Food forms. dosage solid release REFERENCES 3 Hacettepe University, Faculty ofPharmacy, DepartmentofPharmaceutical Technology, 06100Ankara,Türkiye 1 COMPARISON OF DISSOLUTION PROFILES OF TWO COMMERCIALLY COMMERCIALLY TWO OF PROFILES DISSOLUTION OF COMPARISON İnönü University, Faculty ofPharmacy, DepartmentofPharmaceutical Technology, 44280Malatya, Türkiye substance from the drug product, the dissolution drug of release the on depends administration rug absorption from a solid dosage form after oral Müge GENEŞ 2 İnönü University, Faculty ofPharmacy, Undergraduate Student,44280Malatya, Türkiye International Symposium onDrugResearch &Development 2011 AVAILABLE FUROSEMIDE TABLETS FUROSEMIDE AVAILABLE 1 , Naile ÖZTÜRK www.fda.gov/cder/ * [email protected] 2,* DRD 2011 , Mustafa SinanKAYNAK P-107

162 - - - 3. 2. < 5andf the test and reference products were condidered similar (f similar condidered were products reference and test the for obtained furosemide of profiles dissolution results, our on Based similar. are formulations the that considered is it ity ity (f weretablets similar comparedusing the by profilesof lease re Drug nm. 339.5 at spectrophotometer by determined dissolution medium, the concentrations of Furosemide were the with samples the of dilution and filtration After volume. total constant a maintain to medium fresh of volume equal an with replaced and withdrawn was mL) (2 sample min), 60 and 50 40, 30, 20, 10, (5, intervals time predetermined at experiments, all In 29. USP to according freshly prepared the paddle rotation speed was kept at 50 rpm. The buffer was and mL) (900 medium dissolution the as used were phate phos- 5.8 pH 0.5°C. ± 37 at replicates six with method) dle (pad- II Apparatus USP using conducted were tablets 40mg) f 1 Brater DC. Pharmacology of diuretics, Am J Med Sci 319: Sci Med J Amdiuretics, of Pharmacology DC. Brater of investigation the on guidance for Note CPMP EMEA: 38-50, 2000 bioavailability andbioequivalence, CPMP, July2001. If a f a If Dissolution studies on the test (T) and reference (Lasix® reference and (T) test the on studies Dissolution = 2 ) and difference (f ⎣ ⎢ ⎢ ⎢ ⎡ t Σ = n 1 1 value is between 0-15 or f or 0-15 between valueis t R Σ 2 = n 1 t >50). R − t T t ⎦ ⎥ ⎥ ⎥ ⎤ x 100 1 ) factors equations were given below. 1 f 2 , SelmaŞAHİN = 50 x log 2 ⎩ ⎪ ⎨ ⎪ ⎧ value is between 50-100 between valueis ⎣ ⎢ ⎡ 1 + 1 n ∑ t = n 1 3 R t − T t ⎦ ⎥ ⎤ − 0 . 5 x 100 ⎭ ⎪ ⎬ ⎪ ⎫ - - 1

POSTER PRESENTATIONS R - N O F H T It was found that R groups which X n Z R + e M - S N tives tives as mushroom tyrosinase inhibitors. Bioorganic & Medicinal Chemistry 18: 6708-6714, 2010. Int J Mol Sci 10: 2440-2475, 2009. In this study, we synthesized new oxazole derivatives. The The derivatives. oxazole new synthesized we study, this In Metal catalyzed synthesis of 2-substitued oxazoles synthesis Metal catalyzed substituents Various R: Kima YJ, Uyamab H. Cell Mol Life Sci 62: 1707, 2005. Mol Life H. Cell Uyamab YJ, Kima Te-Shang C. An updated rewiev of tyrosinase inhibitors. O 4. 5. synthesis synthesis of oxazoles is achieved via nickel-catalyzed cross- - orga various and 2-methylthio-oxazole of reaction coupling oxazoles synthetic our of abilities Inhibiton reagents. no-zinc were initialy investigated in vitro on mushroom tyrosinase using arbutin as the positive control. In conclusion, new se tyrosinase as activity their and prepared were oxazoles of ries inhibitors was examined. than activity inhibitor better shows rings phenolic the on are and methoxy groups. with methyl R groups 163 P-108 DRD 2011 DRD Sevgi NALBANTOĞLU , Sevgi AKIN ŞAKİ, Mustafa Neslihan International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International

xazoles xazoles are an important class of heterocycles that exhibit diverse biological activities. Natural products containing the oxazole substructure Kocaeli University, Faculty of Sciences and Arts, Department of Chemistry, 41380 Kocaeli, Türkiye Kocaeli, 41380 Department of Chemistry, and Arts, of Sciences Faculty University, Kocaeli

SYNTHESIS OF OXAZOLES AS A MUSHROOM TYROSINASE INHIBITORS Xin-Seng Yao, Xin-Seng Yao, Design and synthesis of biphenyl deriva- Kress TJ, Varie DL, Wepsiec JP. J Org Chem 62: 8634, 1997. 8634, 62: Chem Org J JP. Wepsiec DL, Varie TJ, Kress Spectroscopy; John Wiley & Sons: Hoboken, 2003. Wiley Spectroscopy; John REFERENCES Tyrosinase Tyrosinase is a multifunctional copper-containing en- Kai Bao, Yi Dai, Zhi-Bin Zhu, Feng-Juan Tu, Wei-Ge Zhang, Zhang, Wei-Ge Tu, Dai, Yi Zhi-Bin Zhu, Feng-Juan Kai Bao, Anderson Anderson BA, Becke LM, BooherME, Harn RN, NK,Flaugh Taylor Taylor EC, Wipf P. Oxazoles: Synthesis, Reactions, and O 3. 2. 1. zyme, that is, key in melanin biosynthesis, melanisation in an Melanin important in plays plants. animals and browning UV of effects harmful the skinhuman from protecting in role radiation from the sun. Tyrosinase inhibitors can therefore be clinically useful fort the treatment of some - dermatologi In hyperpigmentation. melanin with associated disorders cal addition, these inhibitors are also known tobe useful in - cos after sunburn3-5. and depigmentation whitening metics for have have been shown to exhibit potent as used been have C-2 at enzymemonosubstituted are that Oxazoles properties1. synthetic intermediates in the synthesis of natural products 2. and pharmaceuticals POSTER PRESENTATIONS (blank perfusion medium),was reported. (blank perfusion (test amlodipine matrix biological in red phenol and metoprolol compound), of determination simultaneous the for optimized method, chromatographic liquid reversed-phase study, this In 2. marker permeability high a as (MTP) prolol meto and marker permeability zero a as used is (PHR) red phenol purpose, Forthis compound. test the of comparison for medium perfusion the to added usually are compounds reference studies, perfusion intestinal In muscle1. heart the reducing blood pressure; in angina it increases blood flow to hence resistanceand wall,peripheral decreasing arterial the in muscle smooth the relaxing by acts AML angina. of ment was approximately 8 min. An antiepileptic drug carbamaze drug antiepileptic An min. approximately8 was assay the for time run total and µL 20 was volume jection respectively.MTP and in- PHR TheAML, wavelengthsfor nm mL/min and UV detector was set at 238 nm, 430 nm and 227 1.0 rate flow a at run were Analyses triethylamine. with 7.0 at adjusted was phase mobile of pH v/v). (60:40 mM) (12.5 buffer phosphate and methanol of consisted phase mobile The AML. of quantification and separation the for used was 2. 1. PHENOL RED IN BIOLOGICAL MATRIX FOR INTESTINAL PERFUSION STUDIES A Agata BOGACZ Milani PZ, Valizadeh H, Azarmi Y, Jalali MB, Tajerzadeh H. TajerzadehMB, Y, Azarmi Jalali H, PZ,Valizadeh Milani RP,Estok JE, Connelly D, Frame KR, Fahrbach CB, Levine C A Simultaneous determination of metoprolol, propranolol metoprolol, of determination Simultaneous Stone LR,etal. Clinical Therapeutics 25:35-57,2003. REFERENCES 4 1 Hacettepe University, Faculty ofPharmacy, DepartmentofPharmaceutical Technology, 06100Ankara, Türkiye SIMULTANEOUS DETERMINATION OF AMLODIPINE, METOPROLOL AND İnönü University, Faculty ofPharmacy, Undergraduate ERASMUSExchange Student,44280Malatya, Türkiye 18 oun Peoee™ ua 5x.0 m 5µm) mm 150x4.60 Luna (Phenomenex™ column 2 İnönü University, Faculty ofPharmacy, DepartmentofAnalytical Chemistry, 44280Malatya, Türkiye sd s n nihpresv ad n h treat the in and anti-hypertensive an as used blocker channel calcium long-acting a is leate) ma- or mesylate besylate, (as (AML) mlodipine * Permenant address: Jagiellonian University, Faculty ofPharmacy, Undergraduate Student, 3 İnönü University, Faculty ofPharmacy, DepartmentofPharmaceutical Technology, 1,*,** International Symposium onDrugResearch &Development 2011 , MichałSTELMASİŃSKİ ** [email protected] 30-690 Krakow, Poland 44280 Malatya, Türkiye Selma ŞAHİN P-109 DRD 2011 1,* 164 , EbruBÜYÜTUNCEL - - - Figure 1.HPLC chromatogram ofMTP, PHR,CBZandAML. the analysis ofAML insamplesofspikedGolytely solution. for applied successfully was method The methods. graphic chromato quantitative the for FDA by suggested limits test suitability system the fulfilled completely analysis the used, conditions chromatographic the Under µg/mL. of 80.0 to range 10.0 concentration the in linear was method The 1). (Figure respectively minutes, 7.5 and 5.4 2.9, 2.1, at eluted and 10µg/mLfor CBZ. MTP PHR, AML, for µg/mL 60 of concentrations at mannitol) NaCl, 10 mM KCl, 40 mM Na encecompounds were intospiked mM (25 solution Golytely the application of the proposed HPLC method, test and refer For guideline3. ICH the to according validated was method pine (CBZ) was used as the internal standard. The developed 3. C Sern Cmite 20) Hroie Tripartite Harmonized (2005). Committee Steering ICH ne tee odtos MP PR CZ n AL were AML and CBZ PHR, MTP, conditions, these Under Guideline. fusion studies, DARU 14(2):102-108,2006. per intestinal situ in rat from samples in red phenol and 4 2 , Mustafa SinanKAYNAK 3, 2 SO 4 , 20 mM NaHCO 3 and 80 mM - - - POSTER PRESENTATIONS - Aethionema Aethionema . 1 2 Cruciata articulate ). The spectropho Hypcoum Hypcoum imberbe, Ziziphora capitata, and Funda N. YALÇIN , Funda 2 year student 06100 Ankara, TURKEY 06100 Ankara, student year th scavenging scavenging activity of the MeOH extract of selected - speci es from Turkish Flora (Aethionema dumanii, Trigonella spec, Minuartia hamata, Ajuga chamaepitys tometric 2,2-diphenyl-1-picrylhydrazil (DPPH) method were activity scavenging radical free the test to used dumanii MeOH extract was exhibited the most antioxidant activity with results. - 165 P-110 DRD 2011 DRD , Duygu KAYA 1,* *[email protected] Kağan ATİKELER International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International and here we have tested free radical Hacettepe University, Faculty of Pharmacy, 5 of Pharmacy, Faculty University, Hacettepe 1 any any diseases and degenerative processes can be associated with the overproduction of re active oxygen species including inflammation,

Hacettepe University, Faculty of Pharmacy, Department of Pharmacognosy, 06100 Ankara, TURKEY, 06100 Ankara, Department of Pharmacognosy, of Pharmacy, Faculty University, Hacettepe 2

extracts in vitro ANTIOXIDANT PROPERTIES OF SOME PLANTS FROM TURKISH FLORA 100-107 (2011). REFERENCES

Harput US, Genç Y, Khan N, Saracoglu 5, İ, Rec. Nat. Prod., Y, Harput US, Genç M brain brain ischemia, mutagenesis, dementia and physiological aging. In addition, it is well known the increased amount of free radicals in wounded and inflammated tissues, cancerous cells and organs. For these reasons, several methods have been developed to measure antioxidant activity of the herbal 1. INDEX BAŞAT, Dilara BAŞARAN, Eyüp BAŞAK, Neşe BANOĞLU, Erden BALZARINI, Jan BALCI, Metin AYTEMİR, MutluD. AYTAÇ, S.Peri AYDIN, Sevil AYDINÖZ, Bilal AYDIN, Elanur ATİLA, Alptuğ ATİKELER, Kağan ATALAY, Rengül-Çetin ASLAN, Ali ASAN, Adem ARAIN, Rafee ARABACI, Taner AOUF, Nour-Eddine ALTUN, Yüksel ALTIPARMAK, Gökçe ALTINTOP, MehlikaDilek ALSANCAK, Güleren ALPAN, A.Selcen ALKAN, Erkin ALİ, Atif ALGÜL, Öztekin ALFARANO, Chiara ALASAĞ, Neva ALAGÖZ, MehmetAbdullah AKSAKAL, Sefa AKIN, Mustafa AKHTAR, Naveed AKGÜN DAR, Kadriye AK, Güliz AKDAĞ, Kadriye AKBUĞA, Jülide AKALIN ÇİFTÇİ, Gülşen AFSORDEH, K. ADIYAMAN, Mustafa ACAR, Mustafa Fahir B A International Symposium onDrugResearch &Development 2011 80, 106,107 44, 128,130 122, 123 115, 116 123, 138 102, 124 157, 158 82, 129 73, 77 56, 57 83, 84 45, 48 146, 110 111 147 165 105 126 104 117 163 109 145 76 58 78 34 81 94 94 47 96 87 48 85 32 88 86 86 50 61 CUSSAC, Daniel COCHRAN, Rory CHENG, Woei Ping CANTÜRK, Pakize CAN, ÖzgürDevrim CANKARA PİROL, Şeyma CANBAY, Hale CANAVAR, Pembe Ece ÇELİK, Leman ÇELİK, İsmail ÇANDAR, Dürdane ÇALIŞ, Ünsal ÇALIŞ, Sema ÇALIŞ, Pınar ÇALIŞKAN, Burcu ÇALIŞKAN, Ayfer ÇAĞLAR, Hatice BÜYÜKTUNCEL, Ebru BULANT, Steeve BOURIN, Philippe BOUASIA, Radia BOŞGELMEZ TINAZ,Gülgün BORA, Aykut BOPPANA, Kiran BOLAT, Gülçin BOĞATARKAN, Çağla BOGACZ, Agata BİRİNCİOĞLU, Mustafa BİLGİNER, Sinan BİBEROĞLU, Kevser BEYTÜT, Fatime BERREDJEM, Malika BERBER, İsmet BELLUR ATICI, Esen BEKSAÇ, M.Sinan BEHERA, Jagannath BEE, Tim BEDİR, Erdal BAYRAKTAR, Aygin BAUMSTÜMMLER, Bernd BASU, Arijit DRD 2011 166 Ç C 151, 160,164 137, 138 119, 146 80, 114 15, 23 101 121 110 143 135 138 110 142 160 105 118 140 164 148 157 105 127 152 90, 32 65 21 59 41 32 28 60 99 55 66 77 50 59 60 16 91 60 DURAN, Nizami DUMANLI, Rukiye DUMANLI, Onur DUBEY, P.K. DOĞRUKOL AK, Dilek DOĞAN, Zümrüt DOĞAN, İnciSelin DOĞAN, Ayşegül DİZMAN, Cemil DİRİCAN, Kamile Zümrüt DİRİCAN, Ebubekir DİLBAZ, Nesrin DEMİR ÖZKAY, Ümide DEMİRKAN, Kutay DEĞİM, Zelihagül DALKARA, Sevim DAĞDEVİREN, İnciNejla GEYİKOĞLU, Fatime GESKOVSKI, Nikola GENEŞ, Müge FARSHI, Farhad FABIAN, Walter M.F. ERTÜRK, AliSerol EROĞLU, Hakan ERİŞ, Rümeysa ERGAN, Erdem EREN, Sami ERDOĞDU, Songül ERDEM KURUCA, Serap ERDEM, Arzum ERAÇ, Bayri EL-SALEH, Firas ÇUBUK DEMİRALAY, Ebru ÇONGUR, Gülşah ÇOBAN, Özlem ÇINAR, Ebru ÇELİK, Venhar D G E F 19, 142,143,144 123, 136,137, 92, 93,94,95, 102, 124,141 61, 79,146 112, 114 69, 70 62, 63 103 103 104 159 162 161 139 138 142 85 60 68 79 59 35 27 91 64 96 92 21 17 42 35 59 89 75 88 16 91 80 ındex INDEX 43 91 48 45 71 65 32 43 59 30 30 99 86 59 145 163 108 113 118 133 109 133 148 125 162 112 62, 63 71, 75 116, 117 80, 106, 107 73, 75, 77, 78 103, 125, 131 102, 124, 141 112, 113, 114 69, 70, 71, 72, 97, 98, 122, 137 Ö O N M Zeynep LÜLECİ, LATIF, M. LATIF, MAMOOD, Tariq MAZUOCHIAN, H. Zeliha MERCAN, MERT, Adem MIAS, Céline MUHAMMAD, Haji Ömer MUNZUROĞLU, NARMADHA, M. P. Emirhan NEMUTLU, John L. NITISS, Karin C. NITISS, ONAR, A. Nur ONUR, Mehmet Ali ORUÇ EMRE, Emine Elçin ÖNAL, Zülbiye ÖNDER, Nur İpek ÖNEM, Ebru ÖZASLAN, Mehmet ÖZÇELİK, Berrin ÖZDEMİR, Ahmet ÖZDEMİR, Filiz ÖZDEMİR, Zeynep ÖZDEN, Tuncel ÖZEK, M. Aykut ÖZKAN, Sibel A. Yusuf ÖZKAY, ÖZ, Özlem ÖZTÜRK, Muharrem ÖZTÜRK, Naile ÖZTÜRK, Yusuf MADNİ, Asadullah Sevgi NALBANTOĞLU, ÖZBAŞ TURAN, Suna 83 88 86 88 91 49 61 92 43 48 41 92 82 81 41 69, 45, 69, 127 144 111 165 158 110 116 148 148 155 101 152 45, 48 71, 75 72, 86 56, 57 82, 129 81, 155 59, 120 162, 164 132, 134 124, 141 80, 106, 107 159, 160, 161, 146, 156, 157, 158 L 167 DRD 2011 DRD 70, 71, 72, 73, 74, 75, 76, 77, 78 70, 71, 72, 73, 74, 75, KAPLANCIKLI, Zafer Asım Zafer KAPLANCIKLI, Nurgül KARADAŞ, KARAKAŞ, Zeynep Ayşegül KARAKÜÇÜK İYİDOĞAN, KARAKURT, Arzu KARAKUŞ, Sevgi Nagihan KAYA, Fatma KAYNAK, Sinan Mustafa KAYNAK, Ş.Orçun KALKAN, KARADENİZ, Hakan Gülşah KARAKAYA, KARALI, Nilgün Nuray KARATAŞ, Bekir KARLIĞA, KART, Didem KAUSHİK-BASU, Neerja Duygu KAYA, KELEŞ, M. Sait KHALIQ, Obaid KHAN, Barkat Ali Yücel KADIOĞLU, KHAN, Haji Muhammad Shoaib KILIÇ, Burçin KILIÇ EREN, Mehtap Halil KILIÇ, İbrahim KIRCHHAUSEN, Tomas Didem Leyla KOZACI, İlkay KÜÇÜKGÜZEL, Ş.Güniz KÜÇÜKGÜZEL, Kaan KÜÇÜKOĞLU, KURAL, Cömert KIR, Esengül KIRKPINAR, İsmet KIR, Sedef Faruk Ö. KOÇAK, Bedia KAYMAKÇIOĞLU, KOÇYİĞİT KÜÇÜKKILINÇ, Tuba Emel D. KURTOĞLU, LANGGUTH, Peter 91 92 47 43 29 21 21 45 58 73 94 88 68 25 60, 153 151 120 106 133 149 108 154 140 126 137 42, 47 62, 63 71, 75 97, 98 112, 113 109, 113 102, 141 132, 134 55, 56, 57, 58 156, 157, 158 115, 116, 117 International Symposium on Drug Research & Development 2011 & Development Symposium on Drug Research International I İ J K H QUE, Qamarul Hasan KACAMER, JAHANGIR, Sajid JAHANGIR, Venkatesan JAYAPRAKASH, İÇEN, Irmak IŞIKDAĞ, İlhan IŞIKDAĞ, İDUĞ, Tuğba Şeyda İLTER, İNCESU, Zerrin Gökalp İŞCAN, İŞLER, Derya Ahmet HACIMÜFTÜOĞLU, HA Fahad HASSAN, A. Atilla HINCAL, GÜL, Mustafa Marija GLAVAŠ-DODOV, Mehtap GÖKÇE, Nesrin GÖKHAN KELEKÇİ, Katerina GORAČINOVA, K. GOWTHAMARAJAN, GULFISHAN GÜL, Halise İnci GÜMÜŞEL, Bülent GÜMÜŞ, Fatma Mehmet GÜMÜŞTAŞ, GÜNAL, Selami GÜNER, Özgül GÜNEŞ, H. Semih GÜNEY, Berrak GÜRBÜZ, Hasan GÜREL, Ebru Merve GÜRKAYNAK, GÜRLER, Berrin Şule GÜRSOY, Nilgün GÜVENER DEMİRAĞ, GÜZEL, Yahya INDEX STELMASİŃSKİ, Michał SOYER, Zeynep SÖNMEZ, Mehmet SINHA, BarijN. SIMONOSKA, Maja SICAK, Yusuf SHOAR, M.KARIMI SHANMUGANATHAM, Karthik SEPTİOĞLU, Ebubekir SATILMIŞ, Gökhan SARIKAYA, Görkem SARAÇ, Selma SANKARAN, Vadivelan SALGIN GÖKŞEN,Umut SAĞLAM, Onursal SADAGHIAN, Mohammad RUBIO, JoseMiguel ROUSHANGAR, L. ROTTMANN, NilsWilhelm RONCALLI, Jérôme ROLLAS, Sevim ROGOJINA, Anna REÇBER, Tuba RASOULI, Sohrab RASOOL, Fatima RAMANATHAN, GuruKumarKollongod RAJAVEL, Sankar RAHMAN, Mohammed RAD, J.SOLEIMANI RADIĆ, Zoran QADRI, M.Samiuddin PIZZINAT, Nathalie PIRI, R. PERÇİN ÖZKORUCUKLU, Sabriye PARINI, Angelo PARALI, Tezcan R Q P S International Symposium onDrugResearch &Development 2011 60, 153 46, 150 46, 150 81, 155 132, 164 139 145 119 155 126 149 124 145 108 145 101 145 134 77 21 72 30 79 60 62 20 32 86 30 59 48 16 43 33 32 35 TÜRKÖZ, Yusuf TÜRKÖZ ACAR, Ebru TÜRKEZ, Hasan TÜRELİ, Emre TURAN ZITOUNI, Gülhan TURAN, Atakan TUNCEL, Ercan TÜLÜ, Metin TUĞRAK, Mehtap TOZKOPARAN, Birsen TOPTAN, Suna TOPÇU, Zeki TOGAR, Başak TEMEL, İsmail TEKE, Şenel TAYLOR, Palmer TATAR, Esra TATAR, Abdulgani TAŞLI, Hüseyin TAŞHAN, Emine TAŞDEMİR, Demet TARI, Özden TAN, Gamze TALELE, Tanaji T. TAHIRI, IftikharAhmed TACAL, Özden ŞİMŞEK, Fevziye Ö. ŞIK, Bünyamin ŞEN, Mesut ŞANLI, Senem ŞANLI, Nurullah ŞANLIER, Şenay ŞAKİ, Neslihan ŞAHİN, Selma ŞAHİN, Özge ŞAHİN, NefiseÖzlen ŞAHİN, Fikrettin DRD 2011 168 159, 160,161,162,164 Ş T 83, 84,122,159,161 92, 93,94,95,96 80, 106,107 44, 128,130 83, 84,87 102, 141 159, 161 92, 96 77, 78 43, 47 125 152 129 147 121 101 155 126 155 156 109 163 135 135 68 24 35 58 92 68 74 91 85 99 66 58 YÜZÜAK, Nesrin YURTTAŞ, Leyla YÜKSEL, Atlan YÜCEL, Çiğdem YILMAZ, Şükran YILMAZ, İsmet YILMAZ, Hayriye YILMAZ, Habibe YILDIZ, Bülent Okan YERER, Mükerrem Betül YELEKÇİ, Kemal YAVUZ ERDOĞAN, Behice YASMEEN, Kousar YALOVAÇ ASLAN,Açelya YALÇIN, Funda N. YALÇIN, Bediha YABANOĞLU ÇİFTÇİ, Samiye VISWANATH, B.A. VERSIANI, MohammadAli VENKATESH, Nagasamy VALLE, Anne UZEL, Ataç UYSAL, Şirin UTKU, Semra ULUSOY, Seyhan UL-HASSAN, Shams UĞURLU, Ezgi UÇAR, Gülberk UÇAR, Bercis İmge ZENGİN, Hüseyin ZENGİN, Gülay ZENCİR, Sevil U V Y Z 60, 149,153,154 115, 116,117 89, 90,118 83, 84,87 153, 154 128, 130 127, 165 153, 154 60, 154 67, 68 43, 47 141 114 135 115 131 108 108 101 127 139 140 102 121 60, 64 64 26 18 47 48 65 65 Kurumsal_ilan_210x297.pdf 22.02.2011 02:19:52

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Türkiye’ye değer katıyoruz Sanofi - aventis Grubu olarak 2000’e yakın çalıºanımızla aºı ve ilaçlarımızın yaklaºık %70’ini Türkiye’de üreterek ekonomimize katkı sağlıyoruz. İnsanların yaºamını iyileºtirmek için Türkiye’ye Ar-Ge yatırımı yapıyor, sağlık profesyonellerimize eğitim ve bilimsel destek sunuyoruz.