Abstract
Isoxazoles are a class of five-membered heterocyclic compounds that have gained significant attention in medicinal chemistry due to their diverse biological activities and therapeutic potential. Recent advances in isoxazole chemistry have led to the development of novel synthetic strategies, enabling the creation of a wide array of isoxazole derivatives with enhanced bioactivity and selectivity. This review explores the latest progress in isoxazole synthesis, highlighting key methodologies such as transition metal-catalyzed cycloadditions, green chemistry approaches, and regioselective functionalization techniques. These advances have not only improved the efficiency of isoxazole synthesis but have also facilitated the design of more complex and bioactive derivatives. In addition to their synthetic advances, isoxazoles have demonstrated a broad spectrum of biological activities, including antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects, making them attractive candidates in drug discovery. This review discusses the structural modifications that enhance their pharmacological properties and their potential for developing therapies for diseases such as cancer, neurodegenerative disorders, and infections. Moreover, we examine the emerging trends in isoxazole-based drug discovery, such as the development of multi-targeted therapies and personalized medicine approaches. The evolving role of isoxazoles in drug discovery underscores their continued importance in modern pharmaceutical research and their potential to address unmet medical needs.