PHARMACOLOGICAL PROSPECTS OF 2-AMINOBENZIMIDAZOLES: ADVANCES IN CHEMISTRY, SYNTHESIS, AND THERAPEUTIC POTENTIAL: A REVIEW

Abstract

2-Aminobenzimidazole (2-ABI) derivatives represent a promising class of nitrogen-containing heterocycles with diverse therapeutic potential. Introduction of an amino group at the 2-position of the benzimidazole ring enhances solubility, chemical stability, and biological interactions, making these compounds attractive scaffolds in drug discovery. Owing to their structural similarity with nucleotides and natural biomolecules, 2-ABIs exhibit strong affinity toward multiple biological targets through hydrogen bonding and π–π interactions. A wide spectrum of pharmacological activities has been reported, including antimicrobial, antimalarial, antiparasitic, antileishmanial, anticancer, anti-inflammatory, anticholinesterase, cardioprotective, and neuroprotective effects. Structure Activity Relationship (SAR) studies indicate that strategic substitutions on the benzimidazole nucleus markedly influence potency and selectivity, thereby guiding rational drug design. Several marketed drugs and investigational candidates incorporate the 2-ABI core, highlighting its clinical relevance. Synthetic strategies for 2-ABIs, ranging from classical condensation to modern metal-free protocols, provide efficient access to novel analogs.. Continued exploration of their molecular mechanisms and optimization of lead compounds could accelerate their progression from bench to bedside, positioning 2-ABIs as valuable scaffolds in modern pharmaceutical sciences.