Benzimidazole: A versatile scaffold for drug discovery and beyond – A comprehensive review of synthetic approaches and recent advancements in medicinal chemistry

Abstract

Heterocyclic compounds are foundational in drug discovery, constituting the core structure of approximately 80% of pharmaceuticals. Benzimidazole, in particular, emerges as a critical aromatic heterocyclic system present in natural compounds, playing an indispensable role in medicinal chemistry. Beyond its pharmaceutical importance, benzimidazole demonstrates its versatility across diverse domains, including materials science and a wide spectrum of pharmacological applications, encompassing antiviral, antifungal, antioxidant, and anticancer properties. The prominence of benzimidazole in both biological activities and industrial applications underscores its pivotal role as a versatile heterocyclic scaffold. Its outstanding attributes, such as enhanced bioavailability, stability, and biological activity, have drawn significant attention from both researchers and industries. This comprehensive review delves into various synthetic approaches to benzimidazole synthesis, with a focus on practical and eco-friendly pathways utilizing various catalysts, including biocatalysts, nanocatalysts, and photocatalysts. Additionally, this review sheds light on the recent advancements of benzimidazole across multiple sectors, spanning pharmaceuticals, materials science, agriculture, and coordination chemistry. Finally, this work summarized the major challenges and presents potential directions for future research endeavors in benzimidazole applications within pharmaceuticals, agriculture, and industrial sectors.

Keywords

• Benzimidazole
• Scaffold
• Pharmacological
• Pharmaceutical
• 1,2-diphenylamine (orthophenylenediamine) (OPDA)
• Anticancer