A novel series of 2-ethyl-1-(4-substituted)phenyl-1H-imidazole derivatives was designed, synthesized, and tested for its antibacterial activity against various bacterial strains. Most of the synthesized compounds showed potent inhibition of several Gram-positive and Gram-negative bacterial strains with minimum inhibitory concentration (MIC) values in the range of 4-256 nmol mL-1 in vitro. The compound [2-ethyl-1-(4-pentoxy)phenyl-1H-imidazole] exhibited the most potent inhibitory activity. The MIC of this compound against S. aureus was found to be 8 nmol mL-1, smaller than that of the reference agents, ciprofloxacin and amoxicillin. Furthermore, the compound exhibited modest activity against several bacterial strains in a dose range of 8-256 nmol mL-1.