State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China; School of Pharmacy, Guizhou Medical University, Guiyang, China.
College of Food Science and Technology, Shanghai Ocean University, Shanghai, China.
Eur J Med Chem. 2021 Oct 5;221:113546. doi: 10.1016/j.ejmech.2021.113546. Epub 2021 May 14.
Hydroxypyranone and hydroxypyridinone are important oxygen-containing or nitrogen-containing heterocyclic nucleus and attracted increasing attention in medicinal chemistry and drug discovery over the past decade. Previous literature reports revealed that hydroxypyranone and hydroxypyridinone derivatives exhibit a wide range of pharmacological activities such as antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, antioxidant, anticonvulsant, and anti-diabetic activities. In this review, we systematically summarized the literature reported biological activities of hydroxypyranone and hydroxypyridinone derivatives. In particular, we focus on their biological activity, structure-activity relationship (SAR), mechanism of action, and interaction mechanisms with the target. The collected information is expected to provide rational guidance for the development of clinically useful agents from these pharmacophores.
羟基吡喃酮和羟基吡啶酮是重要的含氧或含氮杂环核，在过去十年中引起了药物化学和药物发现领域的广泛关注。以往的文献报道表明，羟基吡喃酮和羟基吡啶酮衍生物具有广泛的药理活性，如抗菌、抗真菌、抗病毒、抗癌、抗炎、抗氧化、抗惊厥和抗糖尿病活性。在这篇综述中，我们系统地总结了羟基吡喃酮和羟基吡啶酮衍生物的文献报道的生物活性。特别是，我们关注它们的生物活性、构效关系(SAR)、作用机制以及与靶标的相互作用机制。收集到的信息有望为这些药效团开发临床上有用的药物提供合理的指导。
