Chromone Containing Hybrid Analogs: Synthesis and Applications in Medicinal Chemistry

Abstract

The use of privileged scaffolds has proven beneficial for generating novel bioactive scaffolds in drug discovery program. Chromone is one such privileged scaffold that has been exploited for designing pharmacologically active analogs. The molecular hybridization technique combines the pharmacophoric features of two or more bioactive compounds to avail a better pharmacological activity in the resultant hybrid analogs. The current review summarizes the rationale and techniques involved in developing hybrid analogs of chromone, which show potential in fields of obesity, diabetes, cancer, Alzheimer's disease and microbial infections. Here the molecular hybrids of chromone with various pharmacologically active analogs or fragments (donepezil, tacrine, pyrimidines, azoles, furanchalcones, hydrazones, quinolines, etc.) are discussed with their structure‐activity relationship against above‐mentioned diseases. Detailed methodologies for the synthesis of corresponding hybrid analogs have also been described, with suitable synthetic schemes. The current review will shed light on various strategies utilized for the design of hybrid analogs in the field of drug discovery. The importance of hybrid analogs in various disease conditions is also illustrated.

Discovery of novel chromone and acrylate‐based pancreatic lipase inhibitors: Molecular modelling, synthesis, and in vitro evaluation for the treatment of obesity

“…The principle heterocyclic ring system present in flavonoids is known as chromone. There are many reports of chromone containing analogues with wide variety of biological activities (Auti et al, 2023b;Gaspar et al, 2014;Keri et al, 2014;Madhav et al, 2022). Many researchers have reported the PL inhibitory effects of chromone and chromanone containing natural products (Rajan et al, 2020;Sridhar et al, 2019).…”