ABSTRACT. In the present study, synthesis, and biological evaluation of some novel derivatives of 2-bromomethyl-benzimidazole were investigated. The structures of the new synthesized compounds were characterized by IR, 1 H-NMR, 13 C-NMR, mass spectrometry and elemental analysis and screened for antimicrobial activity against two Gram-positive strains (Staphylococcus aureus and Bacillus subtilis) and two Gram-negative strains (Escherichia coli and Pseudomonas aeruginosa). Results indicate that new compounds showed moderate to good activity when compared with standard antibiotic Ciprofloxacin and Streptomycin.