Antitubercular and antibacterial activities of isoxazolines derived from natural products: Isoxazolines as inhibitors of <i>Mycobacterium tuberculosis</i> InhA

Isoxazoline derivatives of the natural products eugenol, 1’- S-acetoxychavicol acetate and sclareol are prepared through 1,3-dipolar cycloaddition reactions in an aqueous buffered system. The compounds evaluated for their antitubercular antibacterial activities. Compounds 2, 2a 3f display strong activity with minimum inhibitory concentration values 26.68, 17.89 14.58 µM, respectively. Furthermore, derivative exhibits against Bacillus cereus (minimum value 29.16 µM). demonstrate improvements cytotoxicity, demonstrates improved Isoxazolines derived from exhibit Mycobacterium tuberculosis enoyl-acyl carrier protein reductase (InhA) activity, molecular modelling predicts that they form hydrogen bonding hydrophobic interactions NADH key residues InhA binding site.