Chapleo C B, Myers M, Myers P L, Saville J F, Smith A C, Stillings M R, Tulloch I F, Walter D S, Welbourn A P
J Med Chem. 1986 Nov;29(11):2273-80. doi: 10.1021/jm00161a024.
The synthesis and anticonvulsant activity of a series of 2-aryl-5-hydrazino-1,3,4-thiadiazoles are described. The combination of preferred aromatic substituents in the 2-position coupled with alkyl substitution on the hydrazine moiety led to a number of potent compounds lacking sedation, ataxia, or lethality. 5-(2-Biphenylyl)-2-(1-methylhydrazino)-1,3,4-thiadiazole (4m) represents a new class of anticonvulsant agent and compares favorably with the standard drugs phenytoin, phenobarbital, and carbamazepine.
描述了一系列2-芳基-5-肼基-1,3,4-噻二唑的合成及其抗惊厥活性。2-位上优选的芳族取代基与肼部分上的烷基取代相结合，产生了许多没有镇静、共济失调或致死作用的强效化合物。5-(2-联苯基)-2-(1-甲基肼基)-1,3,4-噻二唑(4m)代表了一类新型抗惊厥剂，与标准药物苯妥英、苯巴比妥和卡马西平相比具有优势。
