Abstract

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.