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.
Bharti et al. (Tue,) studied this question.