Abstract
N-Heterocyclic scaffolds have generated significant interest among medicinal chemists. Among
these potential heterocyclic drugs, benzimidazole and imidazopyridine scaffolds are the most
prevalent. Over the past few decades, it has gained immense attention. Both are important classes
of molecules owing to their wide spectrum of biological activities and clinical applications. Both
are used in fashion design and the development of novel synthetic analogs for various therapeutic
disorders. A wide variety of derivatives have been developed as potential anticancer, antimicrobial,
antiviral, and anti-inflammatory agents in addition to other chemotherapeutic agents. The
benzimidazole core is found in a natural system, displaying a wide range of pharmaceutical
properties, and has gained significant attention in medicinal chemistry, as reported in several full
articles and communications. Imidazopyridines are widely distributed in many pharmacologically
important compounds, as shown by their frequent occurrence in a large number of marketed drug
formulations and drug candidates, as well as in other fields such as material and organometallic
chemistry. These scaffolds have been structurally characterized as ligands that can bind to different
receptor sites for the discovery of various emerging drugs. They act as key pharmacophore motifs
for the identification and optimization of lead structures to increase the medicinal chemistry
toolbox. This review outlines the synthesis and medicinal significance of benzimidazoles and
imidazopyridines for their development as lead molecules with improved therapeutic efficiency.
Here, we cover the various designs used to obtain both heterocycles to establish a relationship
between their combination and biological activities.