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Synthesis and Anticonvulsant Activity Evaluation of 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines
Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2011-09-30 , DOI: 10.2174/157018011796575962
Ming-Xia Song , Chun-Bo Zhang , Xian-Qing Deng , Zhi-Gang Sun , Zhe-Shan Quan

Various 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives (3a-3n) were designed keeping in view the wide bioactivities of 1,2,4-triazoles and their fused heterocyclic derivatives. All target compounds 3a-3n, characterized by IR, 1H-NMR and MS, have been evaluated for their anticonvulsant activity against MES-induced seizures. The pharmacological results showed that most of the compounds displayed some degree of anticonvulsant activity. Among them, 6-(4-chlorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine (3h) was the most promising compound with an ED50 value of 40.9 mg/kg and a PI value of 6.5.



中文翻译:

6-苯基-7H- [1,2,4]三唑[3,4-b] [1,3,4]噻二嗪的合成及抗惊厥活性的评价

考虑到1,2,4的广泛生物活性,设计了各种6-苯基-7H- [1,2,4]三唑并[3,4-b] [1,3,4]噻二嗪衍生物(3a-3n)。 -三唑及其稠合的杂环衍生物。已对所有以IR,1H-NMR和MS为特征的目标化合物3a-3n进行了抗MES诱发癫痫发作的抗惊厥活性的评估。药理结果表明,大多数化合物显示出一定程度的抗惊厥活性。其中6-(4-氯苯基)-7H- [1,2,4]三唑[3,4-b] [1,3,4]噻二嗪(3h)是最有前途的化合物,ED50值为40.9 mg / kg,PI值为6.5。

更新日期:2011-09-30
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