SYNTHESIS, CHARACTERIZATION AND ANTITUBERCULAR ACTIVITY OF NOVEL2, 5-DIMETHYL-4-(ARYL OR HETERO ARYL) SUBSTITUTED ANILINE-1, 3-OXAZOLE DERIVATIVES
Rajesh Kumar Singh, Biswa Mohan Sahoo, Ashish Bhatt and Ravi Kant*
Abstract
Tuberculosis treatment remains a challenge that requires new
antitubercular agents due to the emergence of multidrug-resistant
Mycobacterium strains. This paper describes the synthesis,
characterization and the antitubercular activity of some new 2, 5-
dimethyl-4-(aryl or hetero aryl) substituted aniline-1, 3-oxazole
derivatives, which were synthesized by the C-N coupling (Buchwald
coupling) reaction. This reaction involve coupling of 4-(4-
bromophenyl)-2, 5-dimethyloxazole [obtained by the bromination
reaction of 1-(4-bromophenyl) propan-1-one and further cyclisation
reaction with acetamide under microwave] with substituted aryl or
hetero aryl amine in presence of Tris (dibenzylideneacetone) dipalladium(0), BINAP and
cesium carbonate in toluene. All the synthesized compound were characterized by elemental
analysis, 1H NMR and LCMS and also screened for their in- vitro antitubercular activity
against Mycobacterium tuberculosis.
Keywords: Oxazole, p-bromo phenyl ethanone, acetamide, aniline, and antitubarcular activity.
[Full Text Article]