Benzimidazole을 함유한 [1,2,4]­Triazole 유도체의 합성 및 생물학적 활성

Abstract

[1,2,4]Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1Hbenzimidazoleacetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1Hbenzimidazole1acetic acid, hydrazide (2). 5Benzoimidazol1ylmethyl4H[1,2,4]triazole3thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1Hbenzimidazole1acetic acid, 2[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a6v) were synthesized by general substitution reaction. Compounds (6a6v) were screened for Ttype calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a6v) did not show better activities than control compound, mibefradil.