Chiral benzimidazole derivatives have emerged as a significant class of
compounds in pharmaceutical chemistry due to their wide range of potential biological
and clinical applications. The present study explores the synthesis and biological
potentialities of chiral benzimidazole derivatives, highlighting various synthetic
approaches, including condensation, rearrangement, and green synthesis techniques.
The chiral nature of these compounds, which is pivotal in their interaction with
biological receptors, is discussed with a focus on methods for introducing and
controlling chirality. Recent research findings highlight the remarkable biological
activities of these derivatives, including carbonic anhydrase enzyme inhibition,
antibacterial and antifungal properties, urease inhibition, ORL-1 antagonism,
antitrypanosomal activity, antihypertensive effects, and inhibition of leukotriene
biosynthesis. These activities position chiral benzimidazole derivatives as promising
candidates for developing new therapeutic agents for a range of medical conditions.
This study provides a comprehensive overview of the synthesis strategies and
biological evaluations of chiral benzimidazole derivatives, underscoring their potential
in pharmaceutical applications.
Keywords: Chiral, Condensation, Enantioselective synthesis, Pharmacological activity, Rearrangement.
