Synthesis and screening of 2-benzimidazole derivatives have great important in aromatic heterocyclic chemistry due to its potent biologically actives. Synthesis of a series of novel S & N substituted 1H-benzo[d]imidazole-2-thiol derivativesby the condensation of orthophenylene diamine with potassium ethylxanthate, acetic acid,water and subsequent reaction with 2-bromo-1-(4-(trifluoromethyl)phenyl)ethanone,1-bromo-3-(bromomethyl)-5-fluorobenzene,7-(4chlorobutoxy)quinolin-2(1H)-one,1-(bromomethyl)naphthalene, 1-(2-bromoethoxy)-4-nitrobenzeneto get substituted derivatives, Some of them derivatives at NH with methylchloroformates, ethylchloroformate and methyl iodide. Analytical Characterization was performed by Melting point, CHN, IR, NMR and Mass spectral Study. All the compounds synthesized were screened for their potential anti-microbial activity. This exhibited some promising results towards testing organism in-vitro.