AUTHOR=Lin Shibo , Liu Chun , Zhao Xiaotian , Han Xiao , Li Xuanhao , Ye Yongqin , Li Zheyu 

TITLE=Recent Advances of Pyridinone in Medicinal Chemistry

JOURNAL=Frontiers in Chemistry

VOLUME=Volume 10 - 2022

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.869860

DOI=10.3389/fchem.2022.869860

ISSN=2296-2646

ABSTRACT=Pyridinones have been adopted as an important block in medicinal chemistry that could serve as hydrogen-bond donors and acceptors. With the help of feasible synthesis routes via established condensation reactions, the physicochemical properties of such a scaffold could be manipulated by adjustment of polarity, lipophilicity and hydrogen bonding, and eventually lead to its wide application in fragment-based drug design, biomolecular mimetics and kinase hinge-binding motifs. In addition, most pyridinone derivatives exhibit various biological activities ranging from antitumor, antimicrobial, anti-inflammatory, anticoagulant to cardiotonic effect. This review focuses on recent contributions of pyridinone cores to medicinal chemistry, and addresses the structural features and structure-activity relationships (SARs) of each drug-like molecule. These advancements contribute to an in-depth understanding of the potential of this biologically enriched scaffold and expedite the development of its new applications in drug discovery.