An overview of hydroxypyranone and hydroxypyridinone as privileged scaffolds for novel drug discovery.

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.