Synthesis and biological evaluation of 2-methyl-1H-benzimidazole and 1H-benzimidazol-2-yl-methanol

Abstract

Two benzimidazole derivatives namely 2-methyl-1H-benzimidazole (1) and 1H-benzimidazol-2-ylmethanol (2) were synthesized in high yields by condensing O-phenylenediamine with two different carboxylic acid derivatives: glacial acetic acid and glycolic acid, following a different synthetic protocol. Structures were elucidated by spectroscopic methods. Among the two benzimidazole derivatives synthesized, 2-methyl-1H-benzimidazole (1) showed moderate antioxidant activity with IC50 values of 144.84µg/ml whereas 1H-benzimidazol-2-ylmethanol (2) displayed mild antioxidant activity (IC50 value 400.42 µg/ml). Compound 1 also exhibited prominent cytotoxic activities with the LC50 value of 0.42 µg/ml when compared to the standard vincristine sulphate (LC50 value of 0.544 µg/ ml). It also demonstrated weak antimicrobial activity having 7-8 mm of zone of inhibition.