Design And Synthesis of Novel Benzimidazole Derivatives as Antimicrobial Agents

Abstract

The development of drug-resistant strains of microbes has become very in-depth; hence new antimicrobial agents. A set of new benzimidazole derivatives was designed and prepared in this work to determine their prospects of antibacterial and antifungal effectiveness. The synthetic method consisted in condensing of o-phenylenediamine with carboxylic acids or aldehydes, after the purification and structural analysis which was conducted by TLC, melting point, IR, UV-Vis, and NMR. The antimicrobial potential of the synthesized compounds was determined in vitro by the agar well diffusion technique against various strains of bacteria (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa) and fungi (Candida albicans) and the comparative tests were done using standard drugs (ampicillin and fluconazole). Findings indicated that some of the synthesized derivatives had significant antimicrobial activity whereby BZ-2 and BZ-4 had a very strong effect followed by BZ-4 which recorded the largest inhibitory zones against all test strains. The comparison of activities (Structure-Activity Relationship, SAR) of the compounds has proved the presence of electron-donating groups in combination with electron-withdrawing groups, further, the high activity of the compounds tested was in the case of the electron-donating group of NO 2, in spite of e-w-groups. The work also identifies BZ-4 as a prospective lead in the development of dual-action antimicrobial drugs and the significance of strategic functionalization of active benzimidazoles-based therapeutics.