Abstract

Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group & found in many β-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to posses significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, antiinflammatory activity, antioxidant activity, anticancer activity, CNS activity, antitubercular activity and miscellaneous activities like GABA agonistic activity, inhibitory activity, antihypertensive activity, and glutamate transporter activity. The present review summarizes up to date information of various biological activities of isoxazole analogs.

Highlights

  • Among the wide range of heterocycles that have been explored for developing pharmacologically important molecules, isoxazoles 1a play a significant role in the field of medicinal chemistry

  • Emerging research interest on isoxazole moiety already has been proven by various search groups in the literature

  • The great interest associated with isoxazoles and their derivatives is based on their versatility as synthetic building blocks

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Summary

INTRODUCTION

Among the wide range of heterocycles that have been explored for developing pharmacologically important molecules, isoxazoles 1a (fig. 1) play a significant role in the field of medicinal chemistry. Isoxazole derivatives exhibited antibacterial activities in which some compounds are good and some are moderately active when compare with standard drug tested. Bhaskar et al [26] reported the synthesis and antibacterial activities of novel isoxazolidine derivatives 4) by the condensation of different 2-substituted benzimidazole with 3-(2,4-dichlorophenyl)-5methyisoxazole-4-carbonyl chloride and 3-(2,4-dichlorophenyl)-5methylisoxazole-4-carbonyl chloride They evaluated these compounds for their antibacterial and antifungal activities and found that all of them exhibited moderate antimicrobial activity. Rajanarendar et al [33] reported the synthesis and antimicrobial activities of various novel N-protected amino acid/peptide isoxazoles 38 The synthesized compounds are characterized by elemental analysis and spectral studies and evaluated for its antimicrobial activity.

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