M. Arshad, N. Siddiqui, Ahmed Elkerdasy, Abdulmohsen H. Al Rohaimi, S. A. Khan
{"title":"ANTICONVULSANT AND NEUROTOXICITY EVALUATION OF SOME NEWLY SYNTHESIZED THIAZOLYL COUMARIN DERIVATIVES","authors":"M. Arshad, N. Siddiqui, Ahmed Elkerdasy, Abdulmohsen H. Al Rohaimi, S. A. Khan","doi":"10.3844/AJPTSP.2014.132.138","DOIUrl":null,"url":null,"abstract":"The present series of compounds were synthesized with the aim to develop newer anticonvulsant agents that are comparatively more efficacious and safer than the currently used anticonvulsant agents. Various thiazolyl coumarins were synthesized by the reaction of 3-(bromoacetyl)-2H-chromen-2-one with different substituted aryl thiourea. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing Pen Tylenetetra Zole-induced seizure (PTZ) and Maximal Electroshock Seizure (MES) tests at 30, 100 and 300 mg kg-1 dose level. Neurotoxicity and ethanol potentiation test of the compounds were also assessed at the same dose level. Two compounds of the series 3g and 3j exhibited significant anticonvulsant activity at 30 mg kg-1 dose level with lesser neurotoxicity than the standard drug phenytoin.","PeriodicalId":7769,"journal":{"name":"American Journal of Pharmacology and Toxicology","volume":"36 1","pages":"132-138"},"PeriodicalIF":0.0000,"publicationDate":"2014-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"14","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"American Journal of Pharmacology and Toxicology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3844/AJPTSP.2014.132.138","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 14
Abstract
The present series of compounds were synthesized with the aim to develop newer anticonvulsant agents that are comparatively more efficacious and safer than the currently used anticonvulsant agents. Various thiazolyl coumarins were synthesized by the reaction of 3-(bromoacetyl)-2H-chromen-2-one with different substituted aryl thiourea. The structures of the synthesized compounds were confirmed by spectral data and elemental analyses. Compounds were tested for anticonvulsant activity utilizing Pen Tylenetetra Zole-induced seizure (PTZ) and Maximal Electroshock Seizure (MES) tests at 30, 100 and 300 mg kg-1 dose level. Neurotoxicity and ethanol potentiation test of the compounds were also assessed at the same dose level. Two compounds of the series 3g and 3j exhibited significant anticonvulsant activity at 30 mg kg-1 dose level with lesser neurotoxicity than the standard drug phenytoin.
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