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, metal
catalyzed 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.