DOCSLIB.ORG

Studies on the Anthelmintic Property of Aminobenzylated Mannich Bases

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Studies on the Anthelmintic Property of Aminobenzylated Mannich Bases Pharmaceutical Chemistry Studies on the Anthelmintic Property of Aminobenzylated Mannich Bases ChaluvaraMu KC Bhat KI 'HSDUWPHQWRI3KDUPDFHXWLFDO&KHPLVWU\*RYHUQPHQW&ROOHJHRI3KDUPDF\%DQJDORUH,QGLD Address for correspondence:'U.&&KDOXYDUDMX(PDLOFKDOXYDUDMXNF#JPDLOFRP ABSTRACT Studies were conducted on the anthelmintic property of about 15(e-h, 1e-1h, 2d-2f and 3e-3h) synthesized DPLQREHQ]\ODWHG0DQQLFKEDVHVEHDULQJ1PHWK\OSLSHUD]LQHXVLQJ,QGLDQHDUWKZRUPVPheritima posthuma DJDLQVWSLSHUD]LQHFLWUDWHDVVWDQGDUGUHIHUHQFH7KUHHFRQFHQWUDWLRQVRIHDFKFRPSRXQG ZY were studied, which involved the determination of paralysis and death time of the worms. The compound 1g H[KLELWHGWKHPRVWVLJQL¿FDQWDQWKHOPLQWLFDFWLYLW\DPRQJDOOWKHFRPSRXQGVVFUHHQHGDJDLQVWWKHZRUPVDV compared to standard drug. Key words: $PLGHVDPLQREHQ]\ODWHG0DQQLFKEDVHVDQWKHOPLQWLFSURSHUW\Pheritima posthuma, piperazine citrate INTRODUCTION DSRWRVLVHWFDQGWKHEHQ]LPLGD]ROHLPLGD]RWKLD]ROH DQGPDFURF\FOLFODFWRQHV·FODVVRI GUXJVKDYHEHFRPHD Diseases caused by helminth parasites in livestock global phenomenon in gastrointestinal nematodes of farm continue to be a major productivity constraint, especially animals, hence there is a need for an anthelmintic with VPDOOUKPLQDQWVLQWKHWURSLFVDQGVXEWURSLFV,QIHFWLRQV OHVVHUVLGHHIIHFWV$OVRGXHWRHVFDODWLQJFRVWVRI UHVHDUFK by gastrointestinal helminth parasites of livestock are and development and limited commercial attractiveness, among the most common and economically important investment in research for new drug development for GLVHDVHVRI JUD]LQJOLYHVWRFN[1]9DULRXVGUXJVXVHGIRUWKH tropical diseases is much less as compared to other cure of helminth infections are triimidazoles, bithional, GLVHDVHV parabendazole, mebendazole, oxfendazole, niclosamide DQGSLSHUD]LQHHWF+RZHYHUGUXJVOLNHPHEHQGD]ROH ,WLVZHOOGRFXPHQWHGLQWKHOLWHUDWXUHWKDW0DQQLFKEDVHV have considerable side-effects such as mitotic arrest and are known to possess pharmacologically proven therapeutic potentials[2]DQGWKH\ÀQGDSSOLFDWLRQDVDQWLPLFURELDO[3] Access this article online antitubercular,[4] antimalarial,[5] anticancer[6] and local 4uicN Response Code: DQHVWKHWLFGUXJV[7] Though extensive research work has Website: www.jyoungpharm.in EHHQUHSRUWHGRQ0DQQLFKEDVHVUHODWLYHO\YHU\OLWWOHLV NQRZQVRIDUDERXWDPLQREHQ]\ODWHG0DQQLFKEDVHV[8,9] of DOI: 1PHWK\OSLSHUD]LQHDQGWKHOLWHUDWXUHUHYLHZUHYHDOHGWKDW 10.4103/0975-1483.83775 piperazine and related compounds are known to possess DQWKHOPLQWLFDFWLYLW\[10] This enthused us to evaluate some Journal of Young Pharmacists Vol 3 / No 3 243 Chaluvaraju and Bhat: Anthelmintic activity of aminobenzylated Manich bases of the synthesized[11-14] DPLQREHQ]\ODWHG0DQQLFKEDVHV UHDGLQJZDVWDNHQLQWULSOLFDWH 7KHWLPHWDNHQE\ZRUPV >)LJXUH@IRUDQWKHOPLQWLFSURSHUW\LQWKHSUHVHQWVWXG\ to become motionless was noted as paralysis time and to $QWKHOPLQWLFDFWLYLW\RI WKHV\QWKHVL]HGFRPSRXQGV 7DEOH$QWKHOPLQWLFDFWLYLW\RIFRPSRXQGV HKH KGIHK The study of anthelmintic activity was carried out according Test compound &RQFHQWUDWLRQ Time in minutes WRWKHPHWKRGRI $MDLJHRED[15]XVLQJ,QGLDQHDUWKZRUP )RUSDUDO\VLV For death Pheritima posthuma due to its anatomical and physiological Control (Normal saline) 0.9 – – resemblance with the intestinal round worm parasites of Piperazine citrate(Std) 0.1 52 80 [16,17] 0.2 43 75 KXPDQEHLQJV Pheritima posthuma of nearly equal size 0.3 35 66 FP ZHUHFROOHFWHGIURPZDWHUORJJHGDUHDVRI IRUW e 0.1 94 130 ODNHLQ0DQG\DGLVWULFW.DUQDWDND,QGLDIRUWKHSUHVHQW R = -NHCONH- 0.2 82 121 VWXG\ R2 = P-N (CH3)2 0.3 70 109 f 0.1 99 129 R = -NHCSNH- 0.2 91 120 MATERIA/S AND MET+ODS R2 = P-N (CH3)2 0.3 83 107 g 0.1 91 131 3UHSDUDWLRQRI VDPSOHVROXWLRQV R =-NHCOCH3 0.2 83 118 R2 = P-N (CH3)2 0.3 78 105 The suspensions of the sample[18] ZYZYDQG h 0.1 102 142 R =-NHCOC H 0.2 96 131 ZY ZHUHSUHSDUHGE\WULWXUDWLQJWKHFRPSRXQGVZLWK 6 5 R = P-N (CH ) 0.3 84 119 GLVWLOOHGZDWHUDQGZYWZHHQDQGIXUWKHUWUDQVIHUUHG 2 3 2 WRDEHDNHUODEHOHGDVDQGUHVSHFWLYHO\VWLUUHG 1e 0.1 86 135 R = NHCONH- 0.2 79 129 IRUDERXWPLQDWURRPWHPSHUDWXUH7KHUHVXOWLQJVROXWLRQV R2 = H 0.3 68 105 ZHUHWKHQXVHGIRUDQWKHOPLQWLFVWXGLHV 1f 0.1 79 125 S 0.2 70 113 Method of testing HH|| R = ----NCN )LIW\ÀYHJURXSVRI DSSUR[LPDWHO\HTXDOVL]HG FP R = H 0.3 61 100 1g 0.1 68 110 ,QGLDQHDUWKZRUPVPheritima posthama consisting of six R = NHCOCH 0.2 53 99 earthworms in each group were placed in Petri dishes 3 R2 = H 0.3 49 87 µVL]H FRQWDLQLQJVXVSHQVLRQVRI VSHFLÀFFRQFHQWUDWLRQ 1h 0.1 72 121 ZY DWURRPWHPSHUDWXUH(DFKJURXS R = -NHCOC6H5 0.2 63 115 R = H 0.3 56 104 ZDVWUHDWHGZLWKRQHRI WKHIROORZLQJFRQWURO ZY 2 WZHHQLQQRUPDOVDOLQH SLSHUD]LQHFLWUDWH 2d 0.1 98 142 R = -NHCOC H N 0.2 91 129 ZYLQQRUPDOVDOLQH GLIIHUHQWFRQFHQWUDWLRQRI 4 3 2 R2 = H 0.3 84 120 FRPSRXQGV UHVSHFWLYHO\ 2e 0.1 115 161 R = -NH COC4H3N2 0.2 108 154 The times taken for complete paralysis and death were R2 =2,5-Dimethoxy 0.3 97 139 UHFRUGHGXVLQJDVWRSZDWFK7KHPHDQSDUDO\VLVWLPH 2f 0.1 111 150 R = - NH COC H N 0.2 102 141 and mean lethal time for each sample was recorded (each 4 3 2 R2 = 4- OH 0.3 93 130 3e 0.1 110 159 R = -NHCONH- 0.2 105 145 R2 = 3-NO2 0.3 97 132 3f 0.1 106 152 S 0.2 95 144 HH|| R = ----NCN R2 = 3-NO2 0.3 83 130 3g 0.1 119 169 R =-NHCOCH3 0.2 112 154 R2 = 3-NO2 0.3 101 138 3h 0.1 119 167 Figure 1: 5EJGOCVKETGRTGUGPVCVKQPQHEQORQWPFU GJGJFH R = -NH COC6H5 0.2 100 159 GJ R2 = 3-NO2 0.3 91 148 244 Journal of Young Pharmacists Vol 3 / No 3 Chaluvaraju and Bhat: Anthelmintic activity of aminobenzylated Manich bases note the death time the earthworms frequently applied with &KLSHOHPH$*XW-5RVHQWKDO-3&KLEDOH.6\QWKHVLVDQGELRORJLFDO HYDOXDWLRQRI SKHQROLF0DQQLFKEDVHVRI EHQ]DOGHK\GHDQG WKLR external stimuli by transferring them to a beaker containing semicarbazone derivatives against the cystiene protease falcipain-2 and a KRWZDWHULQRUGHUWRFKHFNLWVPRUWDOLW\7KHDQWKHOPLQWLF chloroquine resistant strain of Plasmodium falciparum%LRRUJ0HG&KHP activities of the tested compounds on Pheritima posthuma 6KLYDUDPD+ROOD%9HHUHQGUD%6KLYDQDQGD0.3RRMDU\%6\QWKHVLV HDUWKZRUP DUHLQGLFDWHGLQ7DEOH FKDUDFWHUL]DWLRQDQGDQWLFDQFHUDFWLYLW\VWXGLHVRQVRPH0DQQLFKEDVHV GHULYHGIURPWULD]ROHV(XU-0HG&KHP &KDWXUYHGL6&3DWQDLN*.'KDZDQ%1'L[LW9./RFDODQDHVWKHWLF RESU/TS AND DISCUSSION DFWLYLW\RI VRPHSDUDVXEVWLWXWHGDFHWRSKHQRQH0DQQLFKEDVHV,QGLDQ- 3KDUPDFRO The results of the anthelmintic activity exhibited by title 9DVR\D6/&KRYDWLD373XURKLW'+-RVKL6+*UHHQFKHPLVWU\DSSURDFK WRWKHV\QWKHVLVRI SRWHQWLDOO\ELRDFWLYHDPLQREHQ]\ODWHG0DQQLFKEDVHV compound on Pheritima posthumaDUHVKRZQLQ7DEOH WKURXJKDFWLYHK\GURJHQFRPSRXQGV-6HUE&KHP6RF $FORVHULQVSHFWLRQRI GDWDIURPWKLVWDEOHLQGLFDWHVWKDW 1LPDYDW.63RSXW6/9DVR\D6/-RVKL+66\QWKHVLVDQGDQWLPLFURELDO compound 1 g was found to possess markedly higher DFWLYLW\RI VRPHQHZDPLQREHQ]\ODWHG0DQQLFKEDVHV-,QGLDQ&KHP6RF anthelmintic activity than other compounds compared 7KH0HUFN,QGH[$Q(QF\FORSHGLDRI 'UXJV&KHPLFDOVDQG%LRORJLFDOV ZLWKVWDQGDUG%XWDOOWKHRWKHUFRPSRXQGVZHUHIRXQGWR 13thHG:KLWH+RXVH6WDWLRQ1HZ-HUVH\0HUFNDQG&R,QFS possess an interestingly low level of anthelmintic activity, &KDOXYDUDMX.&%KDW.,6\QWKHVLVDQGELRORJLFDODFWLYLW\RI VRPH ZKLFKLVDQRWHZRUWK\IHDWXUHRIWKHSUHVHQWVWXG\ DPLQREHQ]\ODWHG0DQQLFKEDVHVRI EHQ]DOGHK\GH&KHP$VLDQ- &KDOXYDUDMX.&%KDW.,6\QWKHVLVDQGIn-vitro study of novel amino- EHQ]\ODWHG0DQQLFKEDVHVDVDQWLEDFWHULDODJHQWV-,QGLDQ&RXQF&KHP ACKNOW/EDGMENT &KDOXYDUDMX.&%KDW.,6\QWKHVLVDQGDQWLPLFURELDODFWLYLW\RI DPLQREHQ]\ODWHG0DQQLFKEDVHVRI S\UD]LQDPLGH,QW-&KHP7HFK5HV 7KHDXWKRUVZRXOGOLNHWRWKDQNWKH3ULQFLSDO*RYW&ROOHJHRI 3KDUPDF\%DQJDORUHDQG'LUHFWRUDQG3ULQFLSDO1*60,36 &KDOXYDUDMX.&%KDW.,$PLQREHQ]\ODWHG0DQQLFKEDVHVRI DPLGHV 0DQJDORUHIRUSURYLGLQJWKHIDFLOLWLHVWRFDUU\RXWWKHUHVHDUFKZRUN -&KHP3KDUP6FL $MDL\HRED(22QRFKD3$2ODUHQZDMX27In-vitro anthelmintic properties of buchnolzia coriaceae and Gynandropsis gynandra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ite this article as: &KDOXYDUDMX .& %KDW ., 6WXGLHV RQ WKH DQWKHOPLQWLF -RVKL6.RVKDOD17LZDUL3In vitro study of some medicinally important SURSHUW\RIDPLQREHQ]\ODWHGPDQQLFKEDVHV-<RXQJ3KDUPDFLVWV 0DQQLFKEDVHVGHULYHGIURPDQWLWXEHUFXODUDJHQW%LRRUJ0HG&KHP Source of Support: Nil, ConÀict of Interest: None declared. Journal of Young Pharmacists Vol 3 / No 3 245.
Load more

Recommended publications
  • Chemotherapy of Gastrointestinal Helminths
    Chemotherapy of Gastrointestinal Helminths Contributors J. H. Arundel • J. H. Boersema • C. F. A. Bruyning • J. H. Cross A. Davis • A. De Muynck • P. G. Janssens • W. S. Kammerer IF. Michel • M.H. Mirck • M.D. Rickard F. Rochette M. M. H. Sewell • H. Vanden Bossche Editors H. Vanden Bossche • D.Thienpont • P.G. Janssens UNIVERSITATS- BlfiUOTHElC Springer-Verlag Berlin Heidelberg New York Tokyo Contents CHAPTER 1 Introduction. A. DAVIS A. Pathogenic Mechanisms in Man 1 B. Modes of Transmission 2 C. Clinical Sequelae of Infection 3 D. Epidemiological Considerations 3 E. Chemotherapy 4 F. Conclusion 5 References 5 CHAPTER 2 Epidemiology of Gastrointestinal Helminths in Human Populations C. F. A. BRUYNING A. Introduction 7 B. Epidemiological or "Mathematical" Models and Control 8 C. Nematodes 11 I. Angiostrongylus costaricensis 11 II. Anisakis marina 12 III. Ascaris lumbricoides 14 IV. Capillaria philippinensis 21 V. Enterobius vermicularis 23 VI. Gnathostoma spinigerum 25 VII. Hookworms: Ancylostoma duodenale and Necator americanus . 26 VIII. Oesophagostoma spp 32 IX. Strongyloides stercoralis 33 X. Ternidens deminutus 34 XI. Trichinella spiralis 35 XII. Trichostrongylus spp 38 XIII. Trichuris trichiura 39 D. Trematodes 41 I. Echinostoma spp 41 II. Fasciolopsis buski 42 III. Gastrodiscoides hominis 44 IV. Heterophyes heterophyes 44 V. Metagonimus yokogawai 46 X Contents E. Cestodes 47 I. Diphyllobothrium latum 47 II. Dipylidium caninum 50 III. Hymenolepis diminuta 51 IV. Hymenolepis nana 52 V. Taenia saginata 54 VI. Taenia solium 57 VII. Cysticercosis cellulosae 58 References 60 CHAPTER 3 Epidemiology and Control of Gastrointestinal Helminths in Domestic Animals J. F. MICHEL. With 20 Figures A. Introduction 67 I.
    [Show full text]
  • Anthelmintic Resistance of Ostertagia Ostertagi and Cooperia Oncophora to Macrocyclic Lactones in Cattle from the Western United States
    Veterinary Parasitology 170 (2010) 224–229 Contents lists available at ScienceDirect Veterinary Parasitology journal homepage: www.elsevier.com/locate/vetpar Anthelmintic resistance of Ostertagia ostertagi and Cooperia oncophora to macrocyclic lactones in cattle from the western United States M.D. Edmonds, E.G. Johnson, J.D. Edmonds ∗ Johnson Research LLC, 24007 Highway 20-26, Parma, ID, 83660, USA article info abstract Article history: In June 2008, 122 yearling heifers with a history of anthelmintic resistance were obtained Received 15 October 2009 from pastures in northern California and transported to a dry lot facility in southwest- Received in revised form 28 January 2010 ern Idaho, USA. Fifty heifers with the highest fecal egg counts were selected for study Accepted 24 February 2010 enrollment. Candidates were equally randomized to treatment with either injectable iver- mectin (Ivomec®, Merial, 0.2 mg kg−1 BW), injectable moxidectin (Cydectin®, Fort Dodge, Keywords: 0.2 mg kg−1 BW), oral fenbendazole (Safe-Guard®, Intervet, 5.0 mg kg−1 BW), oral oxfenda- Anthelmintic resistance zole (Synanthic®, Fort Dodge, 4.5 mg kg−1 BW), or saline. At 14 days post-treatment, Cattle Bovine nematodes were recovered from the abomasum, small intestine, and large intestine. Par- Nematodes asitism was confirmed in the control group when 10/10 animals were infected with Efficacy adult Ostertagia ostertagi and 9/10 animals with both developing and early L4 stages of Cooperia O. ostertagi. Similarly, 9/10 animals were parasitized with adult Cooperia spp. Fenbenda- Ostertagia zole and oxfendazole efficacy verses controls were >90% against adult Cooperia spp., while moxidectin caused an 88% parasite reduction post-treatment (P < 0.05).
    [Show full text]
  • WO 2012/148799 Al 1 November 2012 (01.11.2012) 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 2012/148799 Al 1 November 2012 (01.11.2012) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 9/107 (2006.01) A61K 9/00 (2006.01) kind of national protection available): AE, AG, AL, AM, A 61 47/10 (2006.0V) AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, (21) International Application Number: DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, PCT/US2012/034361 HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, (22) International Filing Date: KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, 20 April 2012 (20.04.2012) MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, (25) Filing Language: English SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 61/480,259 28 April 201 1 (28.04.201 1) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (71) Applicant (for all designated States except US): BOARD UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, OF REGENTS, THE UNIVERSITY OF TEXAS SYS¬ TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, TEM [US/US]; 201 West 7th St., Austin, TX 78701 (US).
    [Show full text]
  • Modelling for Taenia Solium Control
    PolicyPolicy & practice & practice Modelling for Taenia solium control strategies beyond 2020 Matthew A Dixon,a Uffe C Braae,b Peter Winskill,a Brecht Devleesschauwer,c Chiara Trevisan,d Inge Van Damme,e Martin Walker,f Jonathan I D Hamley,a Sylvia N Ramiandrasoa,g Veronika Schmidt,h Sarah Gabriël,e Wendy Harrisoni & Maria-Gloria Basáñeza Abstract The cestode Taenia solium is responsible for a considerable cross-sectoral health and economic burden due to human neurocysticercosis and porcine cysticercosis. The 2012 World Health Organization (WHO) roadmap for neglected tropical diseases called for the development of a validated strategy for control of T. solium; however, such a strategy is not yet available. In 2019, WHO launched a global consultation aimed at refining the post-2020 targets for control of T. solium for a new roadmap for neglected tropical diseases. In response, two groups working on taeniasis and cysticercosis mathematical models (cystiSim and EPICYST models), together with a range of other stakeholders organized a workshop to provide technical input to the WHO consultation and develop a research plan to support efforts to achieve the post-2020 targets. The workshop led to the formation of a collaboration, CystiTeam, which aims to tackle the population biology, transmission dynamics, epidemiology and control of T. solium through mathematical modelling approaches. In this paper, we outline developments in T. solium control and in particular the use of modelling to help achieve post-2020 targets for control of T. solium. We discuss the steps involved in improving confidence in the predictive capacities of existing mathematical and computational models on T.
    [Show full text]
  • Sheet1 Page 1 a Abamectin Acetazolamide Sodium Adenosine-5-Monophosphate Aklomide Albendazole Alfaxalone Aloe Vera Alphadolone A
    Sheet1 A Abamectin Acetazolamide sodium Adenosine-5-monophosphate Aklomide Albendazole Alfaxalone Aloe vera Alphadolone Acetate Alpha-galactosidase Altrenogest Amikacin and its salts Aminopentamide Aminopyridine Amitraz Amoxicillin Amphomycin Amphotericin B Ampicillin Amprolium Anethole Apramycin Asiaticoside Atipamezole Avoparcin Azaperone B Bambermycin Bemegride Benazepril Benzathine cloxacillin Benzoyl Peroxide Benzydamine Bephenium Bephenium Hydroxynaphthoate Betamethasone Boldenone undecylenate Boswellin Bromelain Bromhexine 2-Bromo-2-nitropan-1, 3 diol Bunamidine Buquinolate Butamisole Butonate Butorphanol Page 1 Sheet1 C Calcium glucoheptonate (calcium glucoheptogluconate) Calcium levulinate Cambendazole Caprylic/Capric Acid Monoesters Carbadox Carbomycin Carfentanil Carnidazole Carnitine Carprofen Cefadroxil Ceftiofur sodium Centella asiatica Cephaloridine Cephapirin Chlorine dioxide Chlormadinone acetate Chlorophene Chlorothiazide Chlorpromazine HCl Choline Salicylate Chondroitin sulfate Clazuril Clenbuterol Clindamycin Clomipramine Clopidol Cloprostenol Clotrimazole Cloxacillin Colistin sulfate Copper calcium edetate Copper glycinate Coumaphos Cromolyn sodium Crystalline Hydroxycobalamin Cyclizine Cyclosporin A Cyprenorphine HCl Cythioate D Decoquinate Demeclocycline (Demethylchlortetracycline) Page 2 Sheet1 Deslorelin Desoxycorticosterone Pivalate Detomidine Diaveridine Dichlorvos Diclazuril Dicloxacillin Didecyl dimethyl ammonium chloride Diethanolamine Diethylcarbamazine Dihydrochlorothiazide Diidohydroxyquin Dimethylglycine
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9,173.403 B2 Rosentel, Jr
    USOO9173403B2 (12) United States Patent (10) Patent No.: US 9,173.403 B2 Rosentel, Jr. et al. (45) Date of Patent: Nov. 3, 2015 (54) PARASITICIDAL COMPOSITIONS FOREIGN PATENT DOCUMENTS COMPRISING MULTIPLE ACTIVE AGENTS, BR PIO403620 A 3, 2006 METHODS AND USES THEREOF EP 83.6851 A 4f1998 GB 2457734 8, 2009 (75) Inventors: Joseph K. Rosentel, Jr., Johns Creek, WO WO 98,17277 4f1998 GA (US); Monica Tejwani, Monmouth WO WO O2/O94233 11, 2002 WO WO2004/O16252 2, 2004 Junction, NJ (US); Arima Das-Nandy, WO WO 2007/O18659 2, 2007 Titusville, NJ (US) WO WO 2008/O3O385 3, 2008 WO 2008/136791 11, 2008 (73) Assignee: MERLAL, INC., Duluth, GA (US) WO WO 2009/O18198 2, 2009 WO WO 2009/027506 3, 2009 WO 2009/112837 9, 2009 (*) Notice: Subject to any disclaimer, the term of this WO WO 2010/026370 3, 2010 patent is extended or adjusted under 35 WO WO2010.109214 9, 2010 U.S.C. 154(b) by 100 days. OTHER PUBLICATIONS (21) Appl. No.: 13/078,496 Notice of Opposition in the matter of New Zealand Patent Applica (22) Filed: Apr. 1, 2011 tion 595934 in the name of Norbrook Laboratories Limited and Opposition thereto by Merial Limited dated Jun. 28, 2014. (65) Prior Publication Data First Supplementary Notice of Opposition in the matter of New Zealand Patent Application 595934 in the name of Norbrook Labo US 2011 FO245191 A1 Oct. 6, 2011 ratories Limited and Opposition thereto by Merial Limited dated Aug. 28, 2014. Second Supplementary Notice of Opposition in the matter of New Related U.S.
    [Show full text]
  • Alpaca and Llama Parasite Treatment
    Alpaca and Llama Parasite Treatment Albendazole (Valbazen) 10mg/kg Do not recommend in pregnancy or for young crias! Much better for killing tapeworms than Fenbendazole. Give orally - 6cc/100 pounds of body weight. Give one dose once per day for three days in a row (max). May need to repeat in two weeks depending on parasite load. May also have an ovacidal effect – meaning that it kills eggs and thus prevents pasture contamination – therefore it is good for isolation pens. Doramectin (Dectomax) 1cc/50 pounds of body weight every 8 weeks. Or give 1cc/70 pounds of body weight every 6 weeks. Give SubQ. (Recommend 20 gauge needle) Primarily for Meningeal Worm prevention. May kill some strongyles. Probably ineffective against most Nematodirus and Trichuris. Ivermectin (Ivomec) 1cc/70 pounds of body weight for Meningeal Worm prevention. Note that efficacy lasts for no more than 4 weeks max! Excellent for mange treatment: Dose at 1cc/50 pounds for mange – 3 days in row, and then repeat one dose in one week. Do not give mange treatment to pregnant females within first 60 days of pregnancy! Give SubQ. (Recommend 20 gauge needle) Probably ineffective in llamas and alpacas for Trichuris, Nematodirus, Moniezia, some strongyles, and liver flukes. You can purchase Ivomec Plus to kill liver flukes. Fenbendazole (Panacur or Safeguard) 20mg/kg or 1cc/10 pounds of body weight Give orally three days in row for Nematodirus. Give orally 5 days in a row and repeat in 2 weeks for Trichuris and Moneizia (tapeworms). This is a very safe drug, even for very young crias and newly pregnant females! Levamisole 8mg/kg Oral drug is safer than the injectible version.
    [Show full text]
  • Geographically Targeted Interventions Versus Mass Drug Administration to Control Taenia Solium Cysticercosis, Peru Seth E
    Geographically Targeted Interventions versus Mass Drug Administration to Control Taenia solium Cysticercosis, Peru Seth E. O’Neal, Ian W. Pray, Percy Vilchez, Ricardo Gamboa, Claudio Muro, Luz Maria Moyano, Viterbo Ayvar, Cesar M. Gavidia, Robert H. Gilman, Armando E. Gonzalez, Hector H. Garcia, for the Cysticercosis Working Group in Peru Optimal control strategies for Taenia solium taeniasis and source of economic harm in rural regions where the cysticercosis have not been determined. We conducted parasite is endemic and of increasing public health a 2-year cluster randomized trial in Peru by assigning 23 concern because of the rapidly growing global de- villages to 1 of 3 geographically targeted intervention ap- mand for pork (4). The United Nations Food and Ag- proaches. For ring screening (RS), participants living near riculture Organization (https://www.fao.org) ranks pigs with cysticercosis were screened for taeniasis; iden- T. solium as a major foodborne parasite on the basis of tifi ed cases were treated with niclosamide. In ring treat- global likelihood of exposure and potential severity ment (RT), participants living near pigs with cysticerco- of infection (5). In the United States, hospitalizations sis received presumptive treatment with niclosamide. In for cysticercosis exceed those for all other neglected mass treatment (MT), participants received niclosamide tropical diseases combined (6). treatment every 6 months regardless of location. In each approach, half the villages received targeted or mass One of the targets of the 2011 World Health Or- oxfendazole for pigs (6 total study arms). We noted sig- ganization roadmap to overcome neglected tropical nifi cant reductions in seroincidence among pigs in all ap- diseases is to validate T.
    [Show full text]
  • Broad-Spectrum Anthelmintics
    Broad-spectrum Anthelmintics The broad-spectrum anthelmintics can be divided into five groups based on chemical structure and mode of action Each are denoted by a colour symbol and identifier as shown below: Group 1 - BZ, Benzimidazole (‘white’). These are effective against nematodes and are ovicidal, although individual generic products may vary in efficacy against some nematode species, particularly N. battus. Most are efficacious against 1-BZ tapeworms. After administration, the 1-BZ passes into the rumen which acts as a reservoir, allowing gradual release into the bloodstream. It is therefore essential the dose is given over the back of the tongue, so it does not bypass the rumen because the longer the 1-BZs remain in the animal the more effective they are. The 1-BZs act by inhibiting tubulin activity in intestinal cells of nematodes or tegumental cells of cestodes, preventing uptake of glucose. There is one 1-BZ anthelmintic (triclabendazole), which is narrow spectrum (liver fluke only) and differs from all the other 1-BZs, in many respects, but is classed with them because of its chemical structure. Group 2 - LV, Levamisole (LV) (‘yellow’) This group now comprises just one active molecule levamisole, an imidazothiazole (2-LV). This acts rapidly on the nerve ganglia of the parasite, causing paralysis. At normal therapeutic dosages, side 2-LV effects are rarely seen, but the therapeutic safety index for 2-LV is low compared to other anthelmintics, so an overdose may occasionally result in the appearance of cholinergic-type symptoms such as salivation, muscular tremors and head shaking. Levamisole is rapidly absorbed and excreted, with most of the dose lost from the system within 24 hours so it is not essential to maintain high concentrations in the sheep for protracted periods.
    [Show full text]
  • 01 Front.Pdf (2.451Mb)
    Copyright is owned by the Author of the thesis. Permission is given for a copy to be downloaded by an individual for the purpose of research and private study only. The thesis may not be reproduced elsewhere without the permission of the Author. VETERINARY ANTHELMINTICS: THEIR EFFICACY AND EFFECTS ON ABOMASAL PHYSIOLOGY A thesis presented in partial fulfilment of the requirements for the degree of MASTER OF VETERINARY SCIENCE in Veterinary Clinical Pharmacology at Massey University NICHOLAS CHARLES WHELAN March 1998 For Pauline, with all my love iii ABSTRACT PART 1. A Review of the Veterinary Anthelmintic Literature A comprehensive review was undertaken of the pharmacology, efficacy, side effects and toxicity of veterinary anthelmintics used against nematode parasites. Anthelmintics reviewed for use in cattle, sheep, goats, horses, dogs and cats include copper, nicotine, arsenic, tetrachlorethylene, phenothiazine, diethylcarbamazine, piperazine, toluene, cyacethydrazide, bephenium, thenium, organophosphates, and methyridine. The review was limited to cattle for the benzimidazoles, pyrantel, morantel, tetramisole, levamisole, avermectin and milbemycins anthelmintics. Efficacy data is provided in a tabular format which classifies each anthelmintic according to method of administration and dose. PART2 Efficacy of two formulations of moxidectin pour-on and the effects of treatment on serum pepsinogen and gastrin levels and tissue gastrin in cattle Three groups of eight yearling Friesian bulls were used to compare the efficacy of two 5 g/L pour-on formulations of moxidectin applied at 1ml/10kg (500 mcg moxidectin per kg bodyweight) in removing naturally acquired gastrointestinal parasites. At slaughter, 14-16 days after treatment, the burdens of Ostertagia spp. and Trichostrongylus axei were significantly lower in both the treated groups versus the controls (P<0.01 ).
    [Show full text]
  • 2.Anthelmintics
    Anthelmintic Anthelmintic or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. They may also be called vermifuges (those that stun) or vermicides (those that kill). Anthelmintics are used to treat people who are infected by helminths, a condition called helminthiasis. These drugs are also used to treat infected animals. Antiparasitics that specifically target worms of the genus Ascaris are called ascaricides. Classification: Benzimidazoles: Albendazole – effective against threadworms, roundworms, whipworms, tapeworms, hookworms Mebendazole – effective against various nematodes Thiabendazole – effective against various nematodes Fenbendazole – effective against various parasites Triclabendazole – effective against liver flukes Flubendazole – effective against most intestinal parasites Abamectin (and by extension ivermectin) - effective against most common intestinal worms, except tapeworms, for which praziquantel is commonly used in conjunction for mass dewormings Diethylcarbamazine – effective against Wuchereria bancrofti, Brugia malayi, Brugia timori, and Loa loa. Pyrantel pamoate – effective against most nematode infections residing within the intestines `Levamisole Salicylanilide – mitochondrial un-couplers (used only for flatworm infections): Niclosamide Oxyclozanide Nitazoxanide – readily kills Ascaris lumbricoides,[5] and also possess antiprotozoal effects[6]
    [Show full text]
  • Oxfendazole Flukicidal Activity in Pigs
    Accepted Manuscript Title: Oxfendazole flukicidal activity in pigs Author: Pedro Ortiz Susana Terrones Mar´ıa Cabrera Cristian Hoban Laura Ceballos Laura Moreno Candela Canton Meritxell Donadeu Carlos Lanusse Luis Alvarez PII: S0001-706X(14)00107-7 DOI: http://dx.doi.org/doi:10.1016/j.actatropica.2014.03.024 Reference: ACTROP 3331 To appear in: Acta Tropica Received date: 27-12-2013 Revised date: 17-2-2014 Accepted date: 28-3-2014 Please cite this article as: Ortiz, P., Terrones, S., Cabrera, M., Hoban, C., Ceballos, L., Moreno, L., Canton, C., Donadeu, M., Lanusse, C., Alvarez, L.,Oxfendazole flukicidal activity in pigs, Acta Tropica (2014), http://dx.doi.org/10.1016/j.actatropica.2014.03.024 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 1 Oxfendazole flukicidal activity in pigs 2 3 1Pedro Ortiz, 1Susana Terrones, 1María Cabrera, 1Cristian Hoban, 2Laura Ceballos, 2Laura Moreno, 4 2Candela Canton, 3Meritxell Donadeu, 2Carlos Lanusse, 2*Luis Alvarez 5 6 1 Laboratorio de Inmunología, Facultad de Ciencias Veterinarias, Universidad Nacional de Cajamarca, 7 Cajamarca, Perú. 8 9 2Laboratorio de Farmacología, Centro de Investigación Veterinaria de Tandil (CIVETAN), CONICET, 10 Facultad de Ciencias Veterinarias, UNCPBA. Campus Universitario, 7000 Tandil, Argentina.
    [Show full text]