Abstract
Tuberculosis (TB), a bacterial infection caused by Mycobacterium tuberculosis (M-TB) is a fatal disease associated with a high degree of mortality. Present work involved synthesis of a series of novel isoxazoline derivatives (ISOA1-ISOA8) the new antitubercular agents using newly synthesized chalcones (CHL1-CHL8). This was done by subjecting the chalcones to a reaction with hydroxylamine hydrochloride in presence of acetic acid and sodium acetate. The structure of the synthesized compounds was elucidated by IR, 1H NMR and mass spectra. In silico studies of isoxazoline were performed for antitubercular activity by using an enoyl acyl carrier protein (EACP) reductase enzyme. Compound ISOA4 exhibited the best interaction among all these compounds having a docking score of -5.94 compared to standard drug pyrazinamide -6.1. Using in vitro models, purified compounds were tested for their antioxidant and antitubercular properties. Compound ISOA5 showed a significant antioxidant activity compared to ascorbic acid as a standard drug. This study claims new isooxazolines to possess high antioxidant and antitubercular potential, however they must be evaluated for preclinical and clinical significance.
Published Version
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