Shanmugasundaram Palani, Vijay Sheela Balakrishnan, Vaishnavi Dubey, Vishwa Muthukumaran, Indhumathy Pugazhendhi
Fused heterocyclic scaffolds appear to be a most developing topic in therapeutic chemistry especially, benzimidazole was a bicyclic compound consists 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.