Abstract: Fused heterocyclic scaffolds appear to be the most developing topic in therapeutic chemistry, especially benzimidazole, is a bicyclic compound consisting of a benzene ring fused to an imidazole ring and found in the tissues of plants and animals (including histidine, purines, and vitamin B12). Also, it plays an important structural role in the preparation of bioactive compounds. Derivatives of benzimidazole have shown therapeutic activity in various applications, including anthelmintic, anti-inflammatory, anticancer, antimicrobial, and antiulcer. The physicochemical properties of benzimidazole have evolved to promote this activity mainly because of their favourable physical features and their ability to function on several functional biological targets. They include hydrogen bonding, π–π stacking, and hydrophobic interactions. More recently, molecular docking studies with their binding affinity and mechanism of action have become known, which further contributes to the rational design of novel drugs. Derivatives of benzimidazole seem to hold considerable potential for multitargeted therapeutic strategies. In this review, we offer an overview of the chemistry, latest biological activities, design techniques, and structure–activity relationship (SAR) data of several analogues derived from benzimidazole.
Palani et al. (2026) studied this question.