Isoxazole – A Potent Pharmacophore

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 and 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 possess significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, anti-inflammatory activity, antioxidant activity, anticancer activity, CNS (central nervous system) activity, antitubercular activity and miscellaneous activities like GABA (γ-amino butyric acid) 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.

Antitumour Activities of Selected Pure Compounds Identified from the Serum of Crocodylus porosus, Malayopython reticulatus, Varanus salvator and Cuora kamaroma amboinensis

“…120µM of Valdecoxib alone exhibited significant growth inhibition activity against MCF7 cells without affecting the normal skin Hacat cells (Table 1). This was consistent with the findings which showed the ability of Valdecoxib, a type isoxazole (Chikkula and Raja, 2017) with COX-2 inhibitor activity, was previously used to treat inflammation, osteoarthritis (Genç et al, 2017) and even cancer (Atukorala and Hunter, 2013;Daniels et al, 2005;Kivitz et al, 2002). COX-2 is an enzyme which was found to be highly expressed in certain types of cancer such as colorectal cancer (Genç et al, 2017;Atukorala and Hunter, 2013;Daniels et al, 2005;Kivitz et al, 2002;Wang and DuBois, 2010 (Genç et al, 2017;Atukorala and Hunter, 2013).…”

Synthesis and Biological Evaluation of Some Novel Mannich Bases of Isoxazoline Derivatives as Possible Antimicrobial Agents

“…flavas (ATCC 9643) by agar well diffusion method, Sabouraud agar medium is used instead of brain heart infusion agar. The method of testing the antifungal activity is same as that adopted for evaluating antibacterial activity [18][19][20][21][22]. Fluconazole was used as the standard and DMSO was used as solvent.…”

The synthetic and therapeutic expedition of isoxazole and its analogs

“…Inspired by these observations, this review summarizes current propensity in the isoxazole synthetic chemistry and divulges the utility of this potent nucleus as a rich source of new compounds having promising biological activities. Although several reviews have been published earlier on isoxazole (Manna et al 2014;Hu and Szostak 2015;Chikkula and Raja 2017;Sysak and Obmińska-Mrukowicz 2017), the focus was either synthetic routes or chemical reactions of the nucleus or the several biological activities of the isoxazole derivatives. Our effort is an exhaustive and systematic compilation of synthetic, as well as therapeutic voyage of isoxazole and its derivatives till now.…”