Vol. 7, Issue 2, Part B (2025)

Benzimidazole is a privileged heteroaromatic scaffold that has contributed to the development of several clinically approved drugs across therapeutic areas. Its bicyclic structure, consisting of a benzene ring fused with an imidazole, enables strong interactions with biomolecular targets via hydrogen bonding, π-π stacking, and hydrophobic interactions. Benzimidazole derivatives have been extensively explored as anthelmintic agents, antifungal drugs, antivirals, anticancer agents, and proton pump inhibitors. This review provides a comprehensive overview of benzimidazole-based drugs, focusing on their pharmacological actions, clinical applications, mechanisms of action, and structural modifications that have contributed to their therapeutic potential. Special emphasis is placed on FDA-approved benzimidazole drugs such as albendazole, mebendazole, thiabendazole, omeprazole, lansoprazole, rabeprazole, and benomyl, among others. The review also discusses challenges, safety concerns, drug resistance, and the future potential of benzimidazole scaffolds in precision medicine.