Benzimidazoles and Imidazo[1,2-a]pyridines : Biological Activities, Method of Synthesis and Perspectives on Combination of Deuce Pharmacophore

Abstract

The N heterocyclic scaffold has generated a lot of interest among medicinal chemists. Of those potential heterocyclic drugs, benzimidazole and imidazopyridine scaffolds are considerably prevalent. They have gained tremendous importance over the past few decades. Both are an important class of molecules due 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 their derivatives have been developed as potential anti-cancer, anti-microbial, anti-viral, and anti-inflammatory besides other chemotherapeutic agents. Benzimidazole core was found in the natural system displaying a wide range of pharmaceutical properties and it gained significant attention in medicinal chemistry reported in several full articles and communications. While imidazopyridines exhibit a vast distribution in many pharmacologically important compounds shown by its 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 are characterized as structurally potential ligands which can bind to different receptor sites for the discovery of various immerging drugs. They act as key pharmacophore motifs for the identification and optimization of lead structures to increase the medicinal chemistry toolbox. The present review outlines the synthesis and the medicinal significance of benzimidazoles and imidazopyridines for their development as lead molecules with improved therapeutic efficiencies. Here, we cover the various design used to obtain both heterocycles to establish a relationship between their combination to features the biological activities.

Design and synthesis of imidazo[1,2‐a]pyridine‐chalcone conjugates as antikinetoplastid agents

“…Imidazo[1,2‐ a ]pyridine is a diversified scaffold present in various marketed drugs such as alpidem, zolpidem (Harrison & Keating, 2005), optically active GSK812397, necopidem and zolimidine. In addition, its derivatives have exhibited various biological activities such as anticancer, analgesic, antipyretic, antiviral including anti‐HIV activities, liver X receptor (LXR) agonists (Singhaus et al., 2010), γ‐secretase modulators (GSMs) (Bischoff et al., 2012), positive allosteric modulators (PAMs) of metabotropic glutamate 2 receptor (Tresadern et al., 2010) and GABAAα 2 /α 3 agonists (Almirante et al., 1965; Coulibaly et al., 2023; Deep et al., 2017; Devi et al., 2016; Goodacre et al., 2006).…”