Exploring USFDA Approved Imidazole Based Small Molecules In Drug Discovery: A Mini Perspective.

In the present work, we have explored the importance of the imidazole ring and its importance in drug discovery, citing the key approvals in the present decade (2013-2024). The pharmacological attribution for the approved drugs revealed that out of 20 approved drugs, 45% of the approvals were made as anti-infectives, followed by approvals under the category of genetic and metabolic disorders, sexual endocrine disorders, anticancer, and to treat blood pressure, gastrointestinal disorders, and neurological conditions. The excretion pattern of these drugs revealed that the drugs are majorly excreted via the fecal route. The chemical analysis showed that pyrrolidine/pyrrole was major heterocycle in approved drugs, followed by indole ring in hybridization. Considering the substitution pattern, most drugs possessed amide, amines, and fluoro group as functional substitution with 2,4-substitution pattern seen in most approved drugs. The article also expanded to cover the synthetic routes, and metabolic routes for this versatile ring system and case studies for its utility to serve as bioisostere in drug discovery. Furthermore, this article also presents the receptor-ligand interactions of imidazole-based drugs with various target receptors. The present article is, therefore, put forth to assist medicinal chemists and chemists working in drug discovery of this versatile ring system.