The synthesis of the final compounds was carried out in three steps. In step I, Benzil, vanillin, ammonium acetate were cyclized to get 4-(4,5-diphenyl 1H-imidazol-2-yl)-2-methoxyphenol (compound 1). In step II compound 1 treated with chloroacetyl chloride to obtain 4-(4,5-diphenyl-1H-imidazole-2-yl) -2-methoxy phenyl chloroacetate (compound 2). In step III compound II reacted with substituted aniline to get target compounds 4-(4,5-diphenyl-1H-imidazole-2-yl)-2-methoxyphenyl-N-substituted aminoacetate (3a-3h). All the title compounds were recognized by FT-IR, H-1-NMR, mass spectroscopy data, and elemental analysis. All the target compounds have been screened for in-vitro antibacterial activity against organisms like S. aureus and E.coli as well as in-vitro antifungal activity against C. albicans. In-vivo antimicrobial evaluation reveals that the compounds 3c, 3f, and 3h registered significant activity at MIC value 15.62 & mu;g/mL.