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A number of N’-(arylmethylidene)-2-(2-methyl-1H-benzimidazol-1-yl)acetohydrazide and 4-aryl-5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-4H-1,2,4-triazole-3-thiol derivatives were synthesized by incorporating various aromatic and heterocyclic substituents on 2-methyl-1H-benzimidazole. The structures of all the synthesized compounds were elucidated based on their elemental analyses and spectral data. The in vitro activities of these compounds against bacteria and fungi were evaluated by the disc diffusion and the minimum inhibitory concentration (MIC) methods. Some of the synthesized derivatives were found to be as active as kanamycin (standard drug).