Issue 54, 2022

Bioactive 2-pyridone-containing heterocycle syntheses using multicomponent reactions

Abstract

2-Pyridone-containing heterocycles are considered privileged scaffolds in drug discovery due to their behavior as hydrogen bond donors and/or acceptors and nonpeptidic mimics, and remarkable physicochemical properties such as metabolic stability, solubility in water, and lipophilicity. This review provides a comprehensive overview of multicomponent reactions (MCRs) for the synthesis of 2-pyridone-containing heterocycles. In particular, it covers the articles published from 1999 to date related to anticancer, antibacterial, antifungal, anti-inflammatory, α-glucosidase inhibitor, and cardiotonic activities of 2-pyridone-containing heterocycles obtained exclusively by an MCR. The discussion focuses on bioactivity data, synthetic approaches, plausible reaction mechanisms, and molecular docking simulations to facilitate comparison and underscore the applications of the 2-pyridone motif in drug discovery and medicinal chemistry. We also present our conclusions and outlook for the future.

Graphical abstract: Bioactive 2-pyridone-containing heterocycle syntheses using multicomponent reactions

Article information

Article type
Review Article
Submitted
07 11 2022
Accepted
30 11 2022
First published
07 12 2022
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2022,12, 35158-35176

Bioactive 2-pyridone-containing heterocycle syntheses using multicomponent reactions

D. Hurtado-Rodríguez, A. Salinas-Torres, H. Rojas, D. Becerra and J. Castillo, RSC Adv., 2022, 12, 35158 DOI: 10.1039/D2RA07056A

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