Recent developments in the utilization of pyridones as privileged scaffolds in drug discovery.

Introduction: Pyridones are six-membered, nitrogen-containing heterocycles, possessing two isomeric forms; these are 2-pyridones and 4-pyridones. Both pyridone rings display unique physicochemical properties including weak alkalinity and dual hydrogen-bond donor/acceptor propensities. These heterocyclic compounds are particularly underlined for their diverse biological effects, including their cytotoxicity activity as well as their antibacterial, antiviral, anti-inflammatory, and anti-fibrotic properties. This versatility has attracted remarkable interest and held promise for addressing the challenges of drug resistance.

Area Covered: This review is the outcome of literature searches conducted on articles published between 2022 and 2025 across several major databases, including PubMed, Scopus, and Web of Science, using specific keywords concerning 'pyridone' and 'bioactivity.' It focuses on the identification of therapeutic targets, the process of molecular mechanisms, and the plausible modes of interaction and binding.

Expert Opinion: Pyridones have been reported to exhibit a wide range of bioactivities by regulating critical signaling pathways that have a diverse influence on downstream gene expression, intracellular enzyme activity and cytoskeletal configuration. They are consequently used as privileged fragments in the design of biologically active molecules with promising application value in pharmaceutical chemistry. Further investigation will be required to enhance drug-like properties. Continuous progress in structure optimization and clinical trial results will help to provide a guideline for future drug candidate discovery.