RECENT PROGRESS IN THE PHARMACOLOGICAL APPLICATIONS AND SYNTHETIC STRATEGIES OF ISOXAZOLE DERIVATIVES

ABSTRACT Isoxazole and its derivatives have emerged as pharmacologically significant heterocyclic compounds exhibiting a broad spectrum of biological activities. The literature review highlights their diverse therapeutic potential, including antibacterial, anticancer, antiplatelet, analgesic, herbicidal, immunomodulatory, anti-inflammatory, anticonvulsant, and antioxidant properties. These biological effects are often attributed to specific substitutions at various positions on the isoxazole ring, which modulate their interaction with biological targets such as kinases, receptors, and enzymes. Notably, some derivatives demonstrate potent cytotoxicity against cancer cell lines, glycoprotein antagonism for antiplatelet effects, and promising GABA-mediated anticonvulsant action. In addition to pharmacological significance, the review also explores a variety of synthetic strategies for isoxazole derivatives. These include solid-phase synthesis, regiospecific reactions, 1,3-dipolar cycloadditions, metalcatalyzed couplings, and microwave-assisted Michael addition methods. The synthetic approaches offer advantages such as high regioselectivity, mild reaction conditions, good yields, and the use of readily available starting materials. Collectively, the review underscores the considerable potential of isoxazole scaffolds in drug development and agrochemical applications, supported by versatile and efficient synthetic methodologies. Keywords: Isoxazole derivatives, Hetero atom drug, Biological significance, Chalcone derivatives, One-pot synthesis, Solid phase synthesis, Regiospecific synthesis, Copper acetylide cycloaddition.