895331-10-9Relevant articles and documents
Synthesis and anticonvulsant activities of some triazolothiadiazole derivatives
Deng, Xian-Qing,Dong, Zheng-Qi,Song, Ming-Xia,Shu, Bing,Wang, Shi-Ben,Quan, Zhe-Shan
experimental part, p. 565 - 573 (2012/09/05)
The present study describes the synthesis and anticonvulsant activity evaluation of 6-substituted-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives (4a-4x) and their partially dehydrogenated products 5,6-dihydro-6-substituted- [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives (5a-5n). The bioevaluation demonstrated that most compounds in the series of 4a-4x exhibited potent anticonvulsant activity in the maximal electroshock test. Among which, 6-(4-chlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (4h) emerged as the most promising candidate on the basis of its favorable ED50 value of 23.7 mg/kg and PI value of 10.8. In addition, the potency of compound 4h against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline in the chemical-induced seizure tests suggested that compound 4h displayed broad-spectrum activity in several models, and it may exert its anticonvulsant activity through affecting the GABAergic system. The anticonvulsant activities of 6-substituted-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazole derivatives (4a-4x) and their partially dehydrogenated products 5,6-dihydro-6-substituted-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives (5a-5n) were evaluated. Most compounds in the series of 4a-4x exhibited potent anticonvulsant activity in the maximal electroshock test. 6-(4-Chlorophenyl)-[1, 2,4]triazolo[3,4-b][1,3,4]thiadiazole (4h) emerged as the most promising candidate on the basis of its favorable ED50 value of 23.7 mg/kg and PI value of 10.8. Copyright
