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, and anticoagulant to cardiotonic effects. 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.

吡啶酮已被用作药物化学中的重要组成部分，可用作氢键供体和受体。借助可行的合成路线通过建立缩合反应后，这种支架的物理化学性质可以通过调节极性、亲脂性和氢键来控制，并最终导致其在基于片段的药物设计、生物分子模拟物和激酶铰链结合基序中得到广泛应用。此外，大多数吡啶酮衍生物表现出各种生物活性，从抗肿瘤、抗菌、抗炎和抗凝血到强心作用。本综述重点关注吡啶酮核心对药物化学的最新贡献，并阐述每种药物样分子的结构特征和构效关系 (SAR)。