In present study ofpotassium ethyl xanthatewas treated with O-pheylenediamine to form 2-mercaptobenzimidazole, which was treated with1-bromo-4-(bromomethyl) benzeneto obtained 2-[(4-bromobenzyl) sulfanyl]-1H-benzimidazole. Using this compound alkylation and acylation done at the benzimidazole –NH position with different alkyl and acyl halide reagent leading to the functionalized derivatives. Newly synthesized derivatives (6a to 6i) have been evaluated on the basis of spectral and analytical data like melting point, IR, 1H-NMR and Mass spectroscopy. All the synthesized compounds were screened for their antimicrobial activity. This displayed some promising results towards testing organism in-vitro.