A. Foroumadi, S. Tabatabai, G. Gitinezhad, M. Zarrindast, A. Shafiee
{"title":"5-芳基-1,3,4-噻二唑衍生物的合成及其抗惊厥活性","authors":"A. Foroumadi, S. Tabatabai, G. Gitinezhad, M. Zarrindast, A. Shafiee","doi":"10.1211/146080800128735430","DOIUrl":null,"url":null,"abstract":"5-Aryl-1,3,4-thiadiazole derivatives were synthesized and tested for anticonvulsant activity using the pentylenetetrazole-induced lethal convulsion test. The results showed that 2-amino derivatives have anticon vulsant activity (LD50 > 500mg kg−1) and this effect was not mediated through benzodiazepine receptors. The fluoro electron-withdrawing substituent on the phenyl ring did not potentiate the activity of the compounds.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"107 1","pages":"31-33"},"PeriodicalIF":0.0000,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"13","resultStr":"{\"title\":\"SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 5-ARYL-1,3,4-THIADIAZOLE DERIVATIVES\",\"authors\":\"A. Foroumadi, S. Tabatabai, G. Gitinezhad, M. Zarrindast, A. Shafiee\",\"doi\":\"10.1211/146080800128735430\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"5-Aryl-1,3,4-thiadiazole derivatives were synthesized and tested for anticonvulsant activity using the pentylenetetrazole-induced lethal convulsion test. The results showed that 2-amino derivatives have anticon vulsant activity (LD50 > 500mg kg−1) and this effect was not mediated through benzodiazepine receptors. The fluoro electron-withdrawing substituent on the phenyl ring did not potentiate the activity of the compounds.\",\"PeriodicalId\":19946,\"journal\":{\"name\":\"Pharmacy and Pharmacology Communications\",\"volume\":\"107 1\",\"pages\":\"31-33\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2000-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"13\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmacy and Pharmacology Communications\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1211/146080800128735430\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmacy and Pharmacology Communications","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1211/146080800128735430","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 13
摘要
合成了5-芳基-1,3,4-噻二唑衍生物,并采用戊四唑致死性惊厥试验检测了其抗惊厥活性。结果表明,2-氨基衍生物具有抗兀蚁活性(LD50 > 500mg kg - 1),且这种作用不通过苯二氮卓类受体介导。苯基环上的氟吸电子取代基没有增强化合物的活性。
SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 5-ARYL-1,3,4-THIADIAZOLE DERIVATIVES
5-Aryl-1,3,4-thiadiazole derivatives were synthesized and tested for anticonvulsant activity using the pentylenetetrazole-induced lethal convulsion test. The results showed that 2-amino derivatives have anticon vulsant activity (LD50 > 500mg kg−1) and this effect was not mediated through benzodiazepine receptors. The fluoro electron-withdrawing substituent on the phenyl ring did not potentiate the activity of the compounds.