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Synthesis, Characterization and Biological Evaluation of Some New Isoxazoline Derivatives
Corresponding Author(s) : Dinesh K. Jain
Asian Journal of Chemistry,
Vol. 25 No. 2 (2013): Vol 25 Issue 2
Abstract
Isoxazoline represents a unique class of nitrogen- and oxygen-containing five-membered heterocycles, a class of compounds of great importance in biological chemistry. Isoxazoline is considered as one of the most potent antimicrobial compound. Isoxazoline derivatives have been found to possess appreciable antitubercular activity against Mycobacterium tuberculosis. The object of antitubercular drug discovery has become a subject of greater challenge due to increasing incidences of tubercular drug resistance. The study aimed to synthesize potent antitubercular isoxazline derivatives. Different substituted isoxazoline derivatives have been synthesized by cyclization of substituted chalcone derivatives in presence of hydroxylamine hydrochloride. Synthesized derivatives were characterized by melting point, TLC, FT-IR, 1H NMR and MS spectroscopy. Synthesized conjugates were evaluated for in vitro antitubercular activity against M. tuberculosis. Comparable antitubercular activity was obtained as compared to isoniazide.
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References
Rakesh, D.Q. Sun, R.B. Lee, R.P. Tangallapally and R.E. Lee, Eur. J. Med. Chem., 44, 460 (2009).
C. Changtam, P. Hongmanee and A. Suksamrarn, Eur. J. Med. Chem, 45, 4446 (2010).
M.A. Ali, M. Shaharyar and A.A. Siddiqui, Eur. J. Med. Chem., 42, 268 (2007).
P.M. Sivakumar, S.P. Seenivasan, V. Kumar and M. Doble, Bioorg. Med. Chem. Lett., 17, 1695 (2007)