Benzimidazole Nucleus as a Privileged Scaffold in Medicinal Chemistry and its Therapeutic Applications

Document Type : Review Articles

Authors

1 organic and medicinal chemistry department, faculty of pharmacy, university of sadat city, menofia.

2 Professor of pharmaceutical chemistry , Faculty of Pharmacy, University of Ain Shams,cairo, Egypt

3 Pharmaceutical and Organic Chemistry Department, Faculty of Pharmacy, University of Sadat City, Menoufia, Egypt.

4 Associate professor at Pharmaceutical Chemistry Department, Faculty of pharmacy, Menoufia University, Shibin ElKom,

Abstract

This review provides a comprehensive overview of benzimidazoles, a crucial class of heterocyclic compounds in medicinal chemistry, and the significant impact of drug repurposing. We highlight the historical importance and diverse biological activities of benzimidazoles, emphasizing their therapeutic applications across multiple fields. The review also explores Structure-Activity Relationship (SAR) studies, illustrating how specific substitutions on the core dictate activity in various therapeutic areas, such as anti-inflammatory, antihypertensive, anthelmintic, anti-ulcer and anticancer agents. The review heavily emphasizes drug repurposing strategy, highlighting its key benefits, classification, examples and challenges. It thoroughly examines successful cases where benzimidazole-based drugs, such as mebendazole, flubendazole, albendazole, and pimozide, have found new applications, especially in cancer treatment, metabolic and infectious diseases management. While acknowledging the inherent challenges, the review stresses drug repurposing's substantial promise for meeting unaddressed medical demands by broadening the uses of existing medications.

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Articles in Press, Accepted Manuscript
Available Online from 23 October 2025
  • Receive Date: 01 September 2025
  • Revise Date: 08 October 2025
  • Accept Date: 23 October 2025