Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India.
Acta Pharm. 2009 Dec;59(4):441-51. doi: 10.2478/v10007-009-0031-x.
Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N'-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100% indicative of the promising nature of the compounds against seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.
从取代的苯乙酮出发，设计并合成了各种 N-(5-氯-6-取代苯并噻唑-2-基)-N'-(取代苯基)-[1,3,4]噻二唑-2,5-二胺 (5a-t)。根据光谱和元素分析确定了所有化合物的结构。所有新合成的化合物都进行了抗惊厥活性筛选，并与标准药物苯妥英钠进行了比较。有趣的是，所有化合物都在 50-100%的范围内显示出对癫痫发作的保护作用，表明这些化合物具有对抗癫痫发作传播的潜在特性。化合物 5b 和 5c 对 MES 诱导的癫痫发作完全有保护作用。
