DOCSLIB.ORG

3Bottor of Vbt'los;Opbp in CHEMISTRY F~F I

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
3Bottor of Vbt'los;Opbp in CHEMISTRY F~F I 5 STUDIES IN CHEMISTRY OF OXYGEN AND NITROGEN HETEROCYCLES THESIS SUBMITTED FOR THE AWARD OF THE DEGREE OF 3Bottor of Vbt'los;opbp IN CHEMISTRY F~F i BY FARHEEN UNDER THE SUPERVISION OF DR. (MRS.) ZEBA N. SIDDIQUI Li DEPARTMENT OF CHEMISTRY ALIGARH MUSLIM UNIVERSITY AUGARH-202 002 (INDIA) 2013 ,~La&1 !.1►,. \ , ,, ally 2014 111111111 11! 11111 11111 II!!! 1111 11 V 18924 INA My L.ovivu~ t cu-eviza- DEPARTMENT OF CHEMISTRY DR ZrEBA N. SI~DrDIQ~I ~us4`;~' Aligarh Muslim University M.Phil., Ph.D. -~~' M y~' Aligarh-202 002 (India) Associate Professor T Ph. (Off) 0571-2703515 (Res) 0571-2702518 ' (Mob) 09412653054 E-mail: siddqui_zeba(a~yahoo.co.in Certificate This is to certify that the thesis entitled "Studies in Chemistry of Oxygen & Nitrogen Heterocycles" submitted for the award of the degree of Doctor of Philosophy (Ph.D.) in Chemistry to Aligarh Muslim University, Aligarh, India, is a record of bonafide research work carried out by Miss. Farheen under my guidance. It is further certified that the thesis embodies the work of candidate herself and has not been submitted for any degree either of this or any other university. The present work is suitable for submission for the above mentioned purpose. (Dr. Zeba N. Siddihui) Supervisor This thesis has benefited greatly .from the support of many people whose contribution in assorted ways to the research and the making of the thesis de.ser'ed special mention. It is a pleasant task to express my thanks to all those who contributed in many wars to the success of this study and made it an unforgettable experience for me. Therefore _first and foremost I pav all my homage and devote my emotions to ALMIGHTY ALLAH "Director of Life" to give a new direction to my study and for making me much capable that I could adopt and finish this huge task. Without whose blessings and benevolence my endeavours wouldn 't have reached to the zenith of success It is with great pleasure and proud privilege that I wish to express from the deepest core of my heart, the feelings of reverence and indebtedness to my respected Guide Dr. (Mrs.) Zeba N. Siddiqui, Associate professor, Department of Chemistry who has helped me at each and even' stage of my research ►cork with patience and enthusiasm. Her expert guidance and vast experience has contributed great extent to complete this work. I am much indebted to her for her faith in me, incessant encouragement, constructive suggestions, inspiring guidance. and everlasting supportive nature throughout the tenure of my research work without which the aims and objectives of the work could not have been achieved. I would like to express my thanks to Prof. Zafar Ahmad Siddiqui, Chairman, Department of Chemistr►• for providing all necessary facilities needed for the completion of my research work. I gratefully acknowledge University Grants Commission, New Delhi for their generous financial assistance, Sophisticated Analytical Instrumentation Facility (SAIFF, Central Drug Research Institute (CDRI) Lucknow and Punjab University Chandigarh for providing spectral data. I would also like to thank my senior Dr. Mohammed .Vusthafa T.A. for his most willing co- operation and comprehensive exchange of ideas during the course of nn research work. 1 would like to convey my pleasant heartily thankfulness to Mr. Vushtaq Ahmad, Area Business Manager, Bangalore, who has been always participating with my problems and disappointments and rebuilt my confidence at appropriate stages that made my research work success. I offrr my heartjull gratitude to Tubassum Aslam and Mohammed Aslam for their help, encouragement and friendship which lighten mti, day and did not make me feel alone in my research work. disappointments and rebuilt my confidence at appropriate stages that made my research work success. 1 offer my hear/full gratitude to Tabassum Aslam and Mohammed As/am for their help encouragement and friendship which lighten my day and did not make me feel alone in my research work 1 render my special and heartful thanks to my lab colleagues Miss. Tabassum Khan, Miss Kulsum. Miss Saima Tarannum and Mr. Nayeem Ahmad who ever stood beside me with their helping hands and moral support. I gratefully thank all for their help & coordination extended by them. I would also thank to Mr. Abdul Mannan for his help at the time of printing and formatting. I express my sincere gratitude Dr. Mohammad Naseeruddin. Assistant Professor, and Dr. Mohd. Fayazuddin, Senior resident, Department of Pharmacology, JNMC, AMU, Aligarh for their guidance and for animal experimental work of the research work. I also thank to Dr. Asad U. Khan, Associate Professor, Interdisciplinary Biotechnology Unit, Aligarh Muslim University Aligarh for carrying out antimicrobial activities. Where would I be without my family? I have no words (astute anything about my parents but at this occasion, I would like to thanks my father Mr. Farooq Ahmad and mother Mrs. Rosh an Ara. without their love, deep n(jection. heartful blessings and ever encouraging moral support it would have been impossible for me to finish my research work. I am equally thankful to my dearest sisters Arshi Farooq and Bushra Farooq for encouraging Inc and providing every help to fulfill my task Special thanks to the newest addition to my family. Mr. Arshad Yusuf my brother in law for providing me with reasons to smile and laugh which I needed often and for his moral support and courage in each moment. Finally, I would like to thank each and every one of them who helped me directly or indirectly during this wonderful and lots of experience gaining journey. I apologize if in any case lam missing out any q1 the names as lam thankful to one and all Farheeri Pref 1: cc the S%nthcas Of hcterocsclie compounds has always drawn the attention of researchers over the ,,I:, ln,11rnl\ bcclal e ilice compounds have played vital roles in biological processes W,chenlicms. pharmaceuticals and also in human life. Therefore, the development of simple, facile, efficient and en' 1ronmentally benign chemical processes or methodologies to synthesize novel heterocycles and their derivatives is one of the major aspects in organic synthesis. The work embodied in this thesis entitled "Studies in Chemistry of Oxygen and Nitrogen heteroc' cle." deals s% itli the design and development of simple and efficient protocol to synthesize new biologically important heteroc\ dlie dens ativ es from cheap and readily available starting materials such as 4-h\droxvCoutuarin. ? t or;vlchrouioac. cltlo:o--tnethvl-l-phenylpyrazole 4- e irhoxaldeh\de and t-norm\ 1indole. To discuss systematically, thesis is divided into five chapters, ssiu:h are as follciw : Chapter I N raiolcs. I'cridine\. (uulnarir,. Chrontones and lndolcs are well known nitrogen and oxygen heterocv'clic compounds which are employed as important skeletons in organic synthesis, medicinal chemistry and pharmacology. Therefore, various applications associated with these molecules motivated Its to ;elect them as potential candidates for the synthesis of novel heterocycles. This chapter contains scope of present work and depicts a comprehensive survey of literature on the synthesis and reactions of starting materials namely, 4-hydrosycoumarin, 3- forme lchroinone, 5-chloro- 3-methyl- I -pnenylpvrazole--4-carboxaldeltvdc, 3-formylindole, which were taken throughout the thesis and for their applications in the synthesis of different five and six membered heterocycles such as !3-enaminones, pyrazoles, pyridines, dicoumarols, chromanones, indolvI chalcone. indolvl pvrazolincs etc. Chapter 2 (t-Enaminones are important synthetic intermediates for the synthesis of various biologically active heterocyclic compounds due to presence of an coin group linked through a C-C to a carbonyl groiry. Thus, due to their in in pharmaceuticals and in organic synthesis as intermediates, in this section, we have described a simpler and clean method for the synthesis of heterocyclic (3- enammones (176a-d) by condensation of heterocyclic methyl ketones (174a-d) with DMF-DMA (175) by thermal heating under solvent- and catalyst-free condition at lower temperature in excellent yields. Attempts were made to synthesize pyrazole (178a-h) and pyrnnyl pyridine derivatives (ISOa-h) by the reaction of~3-enaminone (176a) with different hydrazines (177a-b) and active methylene compounds (179a-h) respectively under thermal solvent-free condition in the presence of NaH504-SiO_, As expected reactions proceeded efficiently and the desired products were obtained in excellent yields. The catalytic system, NaHSO4-SiOo and products were characterized by powder XRD, SEM and EDX and spectral analysis respectively. Chapter 3 Dicoumacul is a naturally occurring anticoagulant drag that functions as a vitamin K antagonist and possesses various other pharmacological activities such as insecticidal, anthelmintic, hypnotic, antifungal, phytoalexin, HIV protcases inhibition. antimicrobial and antioxidant etc. In clinical trials, such compounds have also demonstrated to have some activity against prostate cancer, malignant melanoma and metastatic renal cell carcinoma. Homogeneous catalysis play a key role in the development of greener, more sustainable chemical processes, and are powerful tools for the synthesis of fine chemicals, pharmaceuticals and materials.This chapter is divided into two sections and describes die synthesis of dicomnamis and 2-hydroxy-4-chmmanones in the presence of 7,n[(L)prolinc]'as an efficient, environmentally benign, water-tolerant, Lewis acid catalyst in green solvent. "water" as the reaction medium. Initially. attempt \\ cre made to synthesize dicoumarol derivatives ( 182a—j ) bV the reaction of 4-hydroxvcoumarin (29) with a variety of aromatic heteroaromatic aldehydes (181a—j) in the presence of 5 viol %Zn[(L)proline]2 in rellux water. The products were obtained in excellent yield in a short time period. In order to show the superiority of Zn[(L)proline],:water catalytic system, a model reaction of 4-hydroxycoumarin and 4- hydroxybenzaldehyde was carried out in different catalysts, solvents and with different amount of catalysts.
Load more

Recommended publications
  • WO 2015/072852 Al 21 May 2015 (21.05.2015) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2015/072852 Al 21 May 2015 (21.05.2015) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 36/84 (2006.01) A61K 31/5513 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/045 (2006.01) A61P 31/22 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 31/522 (2006.01) A61K 45/06 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, PCT/NL20 14/050780 KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (22) International Filing Date: MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, 13 November 2014 (13.1 1.2014) PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (25) Filing Language: English TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of regional protection available): ARIPO (BW, GH, 61/903,430 13 November 2013 (13. 11.2013) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (71) Applicant: RJG DEVELOPMENTS B.V.
    [Show full text]
  • The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
    WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters.
    [Show full text]
  • WO 2015/072853 Al 21 May 2015 (21.05.2015) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2015/072853 Al 21 May 2015 (21.05.2015) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 45/06 (2006.01) A61K 31/5513 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/045 (2006.01) A61K 31/5517 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, A61K 31/522 (2006.01) A61P 31/22 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, A61K 31/551 (2006.01) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, (21) International Application Number: KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, PCT/NL20 14/050781 MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (22) International Filing Date: PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, 13 November 2014 (13.1 1.2014) SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, 61/903,433 13 November 2013 (13.
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr
    US008158152B2 (12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr. 17, 2012 (54) LYOPHILIZATION PROCESS AND 6,884,422 B1 4/2005 Liu et al. PRODUCTS OBTANED THEREBY 6,900, 184 B2 5/2005 Cohen et al. 2002fOO 10357 A1 1/2002 Stogniew etal. 2002/009 1270 A1 7, 2002 Wu et al. (75) Inventor: Nageswara R. Palepu. Mill Creek, WA 2002/0143038 A1 10/2002 Bandyopadhyay et al. (US) 2002fO155097 A1 10, 2002 Te 2003, OO68416 A1 4/2003 Burgess et al. 2003/0077321 A1 4/2003 Kiel et al. (73) Assignee: SciDose LLC, Amherst, MA (US) 2003, OO82236 A1 5/2003 Mathiowitz et al. 2003/0096378 A1 5/2003 Qiu et al. (*) Notice: Subject to any disclaimer, the term of this 2003/OO96797 A1 5/2003 Stogniew et al. patent is extended or adjusted under 35 2003.01.1331.6 A1 6/2003 Kaisheva et al. U.S.C. 154(b) by 1560 days. 2003. O191157 A1 10, 2003 Doen 2003/0202978 A1 10, 2003 Maa et al. 2003/0211042 A1 11/2003 Evans (21) Appl. No.: 11/282,507 2003/0229027 A1 12/2003 Eissens et al. 2004.0005351 A1 1/2004 Kwon (22) Filed: Nov. 18, 2005 2004/0042971 A1 3/2004 Truong-Le et al. 2004/0042972 A1 3/2004 Truong-Le et al. (65) Prior Publication Data 2004.0043042 A1 3/2004 Johnson et al. 2004/OO57927 A1 3/2004 Warne et al. US 2007/O116729 A1 May 24, 2007 2004, OO63792 A1 4/2004 Khera et al.
    [Show full text]
  • Psychological Treatments of the Irritable Bowel Syndrome: a Review
    Gut: first published as 10.1136/gut.30.11.1601 on 1 November 1989. Downloaded from Guit, 1989, 30, 1601-1609 Progress report Psychological treatments of the irritable bowel syndrome: a review SUMMARY Psychological treatments are increasingly being used to help patients with the irritable bowel syndrome (IBS), but the efficacy of such treatments is still debated. This review indicates that there are three ways in which they might have been effective in published studies to date; relating bowel symptoms to stress, specific help with psychosocial problems/ relationships and relaxation to decrease anxiety and tension. A close doctor- patient relationship is regarded as central to these therapeutic tasks but the time required to maximise the effectiveness ofthis therapeutic role means that intensive psychological treatment should be reserved for those IBS patients who do not respond to first line standard medical treatment. There are insufficient data to indicate at present which patients are best suited to each form of psychological treatment. There is growing evidence that patients with the irritable bowel syndrome (IBS) may be helped by psychological treatment but the scientific status of the studies to date has been variable and the indications for such treatment have not been sufficiently clear to guide clinicians. In this review, the types of treatment are considered in turn, paying particular attention to the http://gut.bmj.com/ selection of subjects included in each study, the factors related to outcome and those ingredients which seem to be common to the different treatments. Our aim is to answer the questions 'if such psychological treatments work, what is their mode of action?' and 'for which patients should these treatment be recommended?'.
    [Show full text]
  • Antipsychotics for Treatment of Delirium in Hospitalised Non-ICU Patients
    This is a repository copy of Antipsychotics for treatment of delirium in hospitalised non-ICU patients. White Rose Research Online URL for this paper: https://eprints.whiterose.ac.uk/132847/ Version: Published Version Article: Burry, Lisa, Mehta, S.R., Perreault, M.M et al. (6 more authors) (2018) Antipsychotics for treatment of delirium in hospitalised non-ICU patients. Cochrane Database of Systematic Reviews. CD005594. ISSN 1469-493X https://doi.org/10.1002/14651858.CD005594.pub3 Reuse Items deposited in White Rose Research Online are protected by copyright, with all rights reserved unless indicated otherwise. They may be downloaded and/or printed for private study, or other acts as permitted by national copyright laws. The publisher or other rights holders may allow further reproduction and re-use of the full text version. This is indicated by the licence information on the White Rose Research Online record for the item. Takedown If you consider content in White Rose Research Online to be in breach of UK law, please notify us by emailing [email protected] including the URL of the record and the reason for the withdrawal request. [email protected] https://eprints.whiterose.ac.uk/ Cochrane Database of Systematic Reviews Antipsychotics for treatment of delirium in hospitalised non- ICU patients (Review) Burry L, Mehta S, Perreault MM, Luxenberg JS, Siddiqi N, Hutton B, Fergusson DA, Bell C, Rose L Burry L, Mehta S, Perreault MM, Luxenberg JS, Siddiqi N, Hutton B, Fergusson DA, Bell C, Rose L. Antipsychotics for treatment of delirium in hospitalised non-ICU patients. Cochrane Database of Systematic Reviews 2018, Issue 6.
    [Show full text]
  • Plenary Lectures
    ABSTR A CTS PLENARY LECTURES Examples of genetic biomarkers for efficacy are expression of HER2 and trastuzumab, variants of CYP2D6 and tamoxifen, wild-type K-ras and panitumumab and expression and mutations of EGFR and several EGFR- TKIs. Examples of genetic biomarkers for safety are HLA-allelic variants L01. Intoxications with plants and methodologies for the as well as in immune-mediated hypersensitivities and toxicities of abacavir safety assessment of herbal medicines (HLA-B*5701), and carbamazepine (HLA-B*1502). Examples for pharmacogenomic-based dose-prediction to enhance efficacy and improve K. Hostettmann safety are warfarin, tricyclic antidepressants, and efavirenz. These examples Laboratoire de Pharmacognosie et Phytochimie, École de Pharmacie document the continuing development of pharmacogenomics/toxicogenomics Genève-Lausanne, Université de Genève, 1211 Genève 4, Switzerland as an important contributor to improved drug therapy. Since humans exist on Earth, there have been intoxications with plants. Personalized medicine is a strategy to improve clinical outcome by precise Toxic plants were even used to win battles and wars and famous historical diagnosis (e.g. subphenotypes of cancers) by optimizing drug choice and drug figures and artists were victims of plants. It has been rumoured that dose to the problem and need of the individual patient, by taking into account Alexander the Great (356-323 B.C.) was intoxicated by white hellebore the individual’s genome sequence and environmental and host factors. The (Veratrum album, Liliaceae). The painter Vincent Van Gogh (1853-1890) reasonable hope is that this strategy will decrease the number of adverse drug drank frequently alcohol in excess and mainly absinthe prepared from reactions (ADRs) and increase the efficacy of drug therapy.
    [Show full text]
  • Serotonin Heteroreceptor Complexes and Their Integration of Signals in Neurons and Astroglia—Relevance for Mental Diseases
    cells Review Serotonin Heteroreceptor Complexes and Their Integration of Signals in Neurons and Astroglia—Relevance for Mental Diseases Dasiel O. Borroto-Escuela 1,2,3,* , Patrizia Ambrogini 2 , Manuel Narvaez 3 , Valentina Di Liberto 4, Sarah Beggiato 5, Luca Ferraro 6 , Ramon Fores-Pons 1,3, Jose E. Alvarez-Contino 1,7, Alexander Lopez-Salas 1,3, Giuseppa Mudò 4 , Zaida Díaz-Cabiale 3 and Kjell Fuxe 1,* 1 Department of Neuroscience, Karolinska Institutet, 171 77 Stockholm, Sweden; [email protected] (R.F.-P.); [email protected] (J.E.A.-C.); [email protected] (A.L.-S.) 2 Department of Biomolecular Science Section of Morphology, Physiology and Environmental Biology, Campus Scientifico Enrico Mattei, via Ca’ le Suore 2, 61029 Urbino, Italy; [email protected] 3 Facultad de Medicina, Instituto de Investigacion de Málaga, Universidad de Malaga, Campus de Teatinos s/n, 29071 Málaga, Spain; [email protected] (M.N.); [email protected] (Z.D.-C.) 4 Department of Biomedicine, Neuroscience and Advanced Diagnostic (BIND), University of Palermo, 90134 Palermo, Italy; [email protected] (V.D.L.); [email protected] (G.M.) 5 Department of Medical, Oral and Biotechnological Sciences, University of Chieti-Pescara, 66100 Chieti, Italy; [email protected] 6 Department of Life Sciences and Biotechnology and LTTA Center, University of Ferrara, 44121 Ferrara, Italy; [email protected] 7 Department of Education, School of Medicine, Villa Clara University of Medical Sciences, Polyclinic Juan Citation: Borroto-Escuela, D.O.; Bruno Zayas, 52900 Cifuentes, Cuba Ambrogini, P.; Narvaez, M.; Di * Correspondence: [email protected] (D.O.B.-E.); [email protected] (K.F.); Tel.: +46-760396319 (D.O.B.-E.) Liberto, V.; Beggiato, S.; Ferraro, L.; Fores-Pons, R.; Alvarez-Contino, J.E.; Abstract: The heteroreceptor complexes present a novel biological principle for signal integration.
    [Show full text]
  • WO 2020/212952 A1 22 October 2020 (22.10.2020)
    (12) INTERNATIONAL APPLICATION PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization iii iiiii min linn ill II Minim mill ill m International Bureau (10) International Publication Number (43) International Publication Date WO 2020/212952 A1 22 October 2020 (22.10.2020) (51) International Patent Classification: 62/946, 159 10 December 2019 (10. 12.2019) U S A61K 31/675 (2006.01) A61P 25/30 (2006.01) (71) Applicant: COMPASS PATHFINDER LIMITED A61K 31/4045 (2006.01) A61P 25/00 (2006.01) [GB/GB]; 3rd Floor, 1 Ashley Road, Altrincham, Cheshire A61P1/00 (2006.01) A61P 25/06 (2006.01) WA14 2DT (GB). A61P 25/16 (2006.01) A61P25/22 (2006.01) (72) Inventors: LONDESBROUGH, Derek John; 37 Linden (21) International Application Number: Grove, Hartlepool, Durham TS26 9QA (GB). BROWN, PCT/IB2020/053688 Christopher; 30 Cherrytree Gardens, Gateshead, Tyne and (22) International Filing Date: Wear NE9 6TY (GB). NORTHEN, Julian Scott; 36 Hep- 17 April 2020 (17.04.2020) scott Terrace, South Shields, Tyne and Wear NE33 4TH (GB). MOORE, Gillian; 22 Matfen Court, Sedgefield, (25) Filing Language: English Durham TS21 2JB (GB). PATIL, Hemant Kashinath; (26) Publication Language: English 137C Kingston Road, Leatherhead, Surrey KT22 7NT (GB). NICHOLS, David E.; 56702 Nash, Chapel Hill, N C (30) Priority Data: 27517 (US). CROAL, Megan; c/o COMPASS Pathways 62/835,449 17 April 2019 (17.04.2019) U S Limited, 3rd Floor, 1 Ashley Road, Altrincham Cheshire 62/835,450 17 April 2019 (17.04.2019) U S WA14 2DT (GB). ERIKSSON, Hans Ake; c/o COM¬ 62/835,458 17 April 2019 (17.04.2019) U S PASS Pathways Limited, 3rd Floor, 1 Ashley Road, Altrin¬ 62/835,460 17 April 2019 (17.04.2019) U S cham Cheshire WA14 2DT (GB).
    [Show full text]
  • Piperazine Derivatives As Dangerous Abused Compounds
    Acta Pharm. 70 (2020) 423–441 Review https://doi.org/10.2478/acph-2020-0035 Piperazine derivatives as dangerous abused compounds ANNA WELZ* Piperazine derivatives are a group of compounds with a MARCIN KOBA psychostimulant effect. They are an alternative to illegal drugs. They are being searched for recreational use due to Department of Toxicology their psychoactive and hallucinogenic effects. The high Faculty of Pharmacy popularity of these compounds can be noticed all over the Collegium Medicum Nicolaus world due to easy purchase, lack of legal regulations and Copernicus University incorrect assessment of the safety of use. The recreational Bydgoszcz, Poland use of piperazine derivatives can often result in chronic and acute health problems and additionally with unpre- dictable remote effects. It is also common to take mixtures of psychoactive compounds. This hinders the correct diagnosis and treatment of patients with poisoning. The presented work is an illustration of the wide problem of pipe razine derivatives abuse. The health effects and the possi bility of identifying these compounds in preparations and biological material are described. Accepted December 3, 2019 Keywords: piperazine derivatives, designer drugs, benzyl- Published online December 16, 2019 piperazine, phenylpiperazine, addiction INTRODUCTION Available literature data indicates a growing interest in new psychoactive substances (NPS) around the world (1, 2). These products, often called designer drugs, can be divided into three main groups: piperazine derivatives, ketoarylamines and synthetic cannabi- noids. The modified chemical structures of these compounds aim to mimic the pharmaco- logical effects of illicit drugs and trigger potential abuses. The problem of today is consumers experimenting with these substances in order to achieve a specific benefit (3, 4).
    [Show full text]
  • Antidepressant Treatment for Postnatal Depression
    This is a repository copy of Antidepressant treatment for postnatal depression. White Rose Research Online URL for this paper: https://eprints.whiterose.ac.uk/163986/ Version: Published Version Article: Brown, Jennifer Valeska Elli orcid.org/0000-0003-0943-5177, Wilson, Claire A., Ayre, Karyn et al. (5 more authors) (2020) Antidepressant treatment for postnatal depression. Cochrane Database of Systematic Reviews. CD013560. ISSN 1469-493X https://doi.org/10.1002/14651858.CD013560 Reuse Items deposited in White Rose Research Online are protected by copyright, with all rights reserved unless indicated otherwise. They may be downloaded and/or printed for private study, or other acts as permitted by national copyright laws. The publisher or other rights holders may allow further reproduction and re-use of the full text version. This is indicated by the licence information on the White Rose Research Online record for the item. Takedown If you consider content in White Rose Research Online to be in breach of UK law, please notify us by emailing [email protected] including the URL of the record and the reason for the withdrawal request. [email protected] https://eprints.whiterose.ac.uk/ Cochrane Library Cochrane Database of Systematic Reviews Antidepressant treatment for postnatal depression (Protocol) Brown JVE, Wilson CA, Ayre K, South E, Molyneaux E, Trevillion K, Howard LM, Khalifeh H Brown JVE, Wilson CA, Ayre K, South E, Molyneaux E, Trevillion K, Howard LM, Khalifeh H. Antidepressant treatment for postnatal depression. Cochrane Database of Systematic Reviews 2020, Issue 3. Art. No.: CD013560. DOI: 10.1002/14651858.CD013560. www.cochranelibrary.com Antidepressant treatment for postnatal depression (Protocol) Copyright © 2020 The Cochrane Collaboration.
    [Show full text]