Harish K P, Mohana K N, Mallesha L
Bioorg Khim. 2014 Jan-Feb;40(1):108-16. doi: 10.1134/s1068162014010051.
A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives were synthesized by the reaction of 3-(2-cyanopropan-2-yl)-N-(5-(piperazine-1-yl)-1,3,4-thiadiazol-2-yl)benzamide with various sulfonyl chlorides and evaluated for their anticonvulsant activity in MES test. Rotorod method was employed to determine the neurotoxicity. The purity of the compounds is confirmed on the basis of their elemental analysis. The structures of all the new compounds are established on the basis of 1H NMR and mass spectral data. Out of fifteen compounds, three were found to be potent anticolvunstants. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg).
通过3-(2-氰基丙烷-2-基)-N-(5-(哌嗪-1-基)-1,3,4-噻二唑-2-基)苯甲酰胺与各种磺酰氯反应合成了一系列2,5-二取代-1,3,4-噻二唑衍生物，并在最大电休克（MES）试验中评估了它们的抗惊厥活性。采用转棒试验法测定神经毒性。根据元素分析确定化合物的纯度。所有新化合物的结构均根据1H核磁共振（1H NMR）和质谱数据确定。在15种化合物中，有3种被发现是有效的抗惊厥剂。相同的化合物在最大给药剂量（100 mg/kg）下未显示神经毒性。
