Abstract
Isoxazoles are five-membered aromatic heterocyclic compounds in which
oxygen and nitrogen atoms are present at positions 1 and 2 of the ring system.
Isoxazole derivatives play a vital role due to their diverse biological activities, such as
antimicrobial, antifungal, anti-viral, anti-tubercular, anti-epileptic, anti-diabetic,
anticancer, anthelmintic, antioxidant, antipsychotic, antimalarial, analgesic, anti-inflammatory, etc. Isoxazole scaffold is present in various drug molecules, such as
leflunomide (antirheumatic), valdecoxib (non-steroidal anti-inflammatory drug), and
zonisamide (anti-convulsant). Similarly, isoxazole derivatives such as isocarboxazid
act as monoamine oxidase inhibitors. It is used to treat symptoms of depression that
may include anxiety, panic, or phobias. Whereas the isoxazole derivatives, including
sulfamethoxazole, sulfisoxazole, and oxacillin, are used clinically for the treatment of
bacterial infections. Isoxazole pharmacophore is also present in β-lactamase resistant
antibiotics such as cloxacillin, dicloxacillin, and flucloxacillin. Cycloserine is a
naturally occurring antibiotic that possesses isoxazole moiety with anti-tubercular,
activity. This study focuses on the therapeutic potentials of isoxazole derivatives in
new drug development.
Keywords: Biological activity, Disease, Drug, Isoxazoles, Pharmacophore, synthesis.