Exploring Key Microbial Enzymes as Targets for Benzimidazole Derivatives: Synthesis, SAR, and Therapeutic Relevance

Abstract

The benzimidazole pharmacophore has become a key theme in the identification and advancement of innovative antimicrobial agents owing to its resemblance with the purines (nucleotides), which make it responsible for better interaction with the targeted enzymes and receptors. This review thoroughly gives a complete overview in current developments of benzimidazole derivatives as antimicrobial agents. In the present review, we have collected information from various published reports on benzimidazole derivatives as anti‐bacterials by inhibiting DNA gyrase and topoisomerase, peptide deformylase, glucosamine‐6‐phosphate synthase, dihydrofolate reductase, enoyl acyl carrier protein reductase, dehydrosqualene synthase, dihydropteroate synthase, and peptidyl transferase, and as antifungal agents by inhibiting lanosterol 14α‐demethylase. The current review explored the synthesis, structure–activity relationship (SAR), and mechanistic studies of benzimidazole derivatives as antimicrobial agents in the past 11 years (2015–2026). The aim is to assemble the current research reports and to give a generalized view to the medicinal chemists for the design of potent antimicrobials.