Green synthetic approaches to benzimidazole scaffolds: recent advances in antimicrobial and anticancer drug discovery

The growing demand for sustainable and efficient drug development has directed significant attention toward green chemistry in heterocyclic synthesis. Among various pharmacophores, benzimidazole has emerged as a privileged scaffold due to its remarkable structural versatility and broad-spectrum biological activities. The present review highlights recent advances in environmentally friendly synthetic approaches for the synthesis of benzimidazole derivatives and their promising roles in antimicrobial and anticancer drug discovery. Green synthetic strategies such as microwave-assisted reactions, ultrasound irradiation, solvent-free conditions, mechanochemical methods, and the use of recyclable catalysts have revolutionised conventional protocols by reducing reaction time, energy consumption, and hazardous waste generation. These methodologies not only enhance yield and selectivity but also align with the principles of sustainable chemistry. Recent studies demonstrate that structurally diverse benzimidazole derivatives exhibit potent activity against multidrug-resistant microbial strains and various cancer cell lines. The incorporation of different functional groups into the benzimidazole ring has significantly improved pharmacokinetic and pharmacodynamic profiles, emphasising its importance in rational drug design. This review presents a comprehensive overview of green synthetic methodologies alongside structure–activity relationships and biological evaluations of benzimidazole derivatives. It aims to inspire further research toward the development of eco-friendly, cost-effective, and biologically potent therapeutic agents, thereby bridging the gap between sustainable chemistry and modern medicinal needs.