Recent Advances in the Synthesis and Biological Evaluation of Benzimidazole Derivatives: A Review

Author

Prithvi rani AR, Dr. Sebastin V

Abstract

 Benzimidazole, a bicyclic heteroaromatic system formed by fusing benzene and imidazole rings, is a privileged scaffold in medicinal chemistry and is present in several marketed drugs. This review summarises recent developments in benzimidazole synthesis, covering classical condensation, catalytic, green, and multicomponent approaches, and reviews biological evaluation across antimicrobial, antifungal, anticancer, anthelmintic, antiulcer, antihypertensive, antiviral, and anti-inflammatory activities. Mechanisms and structure–activity relationships (SAR) at the C-2, N-1, and C-5/C-6 positions are emphasised. Antimicrobial and antifungal activity is considered in relation to growing resistance, and anticancer activity in relation to tubulin, PARP, and DNA-binding mechanisms. Current limitations include variability between assays, incomplete pharmacokinetic and target-validation data, and few direct comparisons between closely related series. A stepwise evaluation strategy is proposed to move promising derivatives from in silico design to biochemical, cellular, and preliminary pharmacokinetic studies.

Keywords

benzimidazole; privileged scaffold; heterocyclic synthesis; green chemistry; structure–activity relationship; antimicrobial; anticancer

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