Derivatives of benzimidazole containing N-substituted benzyl, benzensuphonyl and acetyl were synthesized from a variety of amino acids such as Lysine and Leucine. The structures of all the synthesized compounds were elucidated by using IR, 1H-NMR, 13C-NMR.The synthesized target compounds were evaluated in vitro antibacterial activity against three bacterial strains by employing the disc diffusion method using Ciprofloxacin as a standard drug. The anti-bacterial assay revealed that the compounds (6’ b) and (6’d) showed better activity 14, 9, 8 and 12, 9, 7 mm zone of inhibition against S. auras, E. coli and K. pneumonia respectively.