Exploring the Role of Benzimidazole-Containing Scaffolds for the Design of New Compounds in Drug Discovery

Introduction: Benzimidazole and its derivatives are among the most popular structures used in pharmaceutical and medicinal chemistry for drug discovery, particularly within the wide variety of heterocycles. Benzimidazole has a preferred structure in drug discovery due to its distinct structural characteristics and the diverse biological actions of its derivatives. Methods: This study highlights the significance of this moiety due to its broad range of biological features and the widespread use of benzimidazole. Results: This review consolidates extensive research conducted from 1990 to 2025, highlighting benzimidazole derivatives as key pharmacophores across diverse therapeutic areas. Benzimidazole compounds exhibit multifaceted anti-inflammatory, analgesic, antiviral, anticancer, antioxidant, and anthelmintic activities, indicating their systemic benefits. Discussion: In many drugs used to treat conditions such as cancer, microbial infections, inflamma-tory disorders, hypertension, and malaria, the benzimidazole ring structure exhibits a broad range of pharmacological activity. Additionally, this fused heterocycle benzimidazole core may interact with various anions and cations, as well as biomolecules, in the human body to produce a range of biological activities, including antidepressant, antiviral, antibacterial, antifungal, anti-inflamma-tory, and analgesic effects. Conclusion: This review focuses on benzimidazole derivatives and their effects on different sites of action, as well as contemporary developments in drug design and development.