Synthesis of N-{5-aryl-1,3,4-oxadiazole-2-yl}methyl-4-methoxyaniline derivatives and their anticonvulsant activity.

摘要

A series of some new 2,5-disubstituted-1,3,4-oxadiazoles 4(a-i) have been conveniently synthesized by intramol. oxidative cyclization of (E)-2-(arylbenzylidene)-2-[(4-methoxyphenyl)amino]acetohydrazides promoted by iodobenzene diacetate as an oxidant. The structures of the synthesized compds. have been confirmed by 1H and 13C NMR, IR, MS and elemental anal. All the newly synthesized compds. were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method. Compds. 4g, 4d and 4a were found to be the most potent of this series. The same compds. showed no neurotoxicity at the max. dose administered. [on SciFinder(R)]