Abstract

FACILE SYNTHESIS, CHARACTERIZATION AND IN VITRO ANTI-TUBERCULAR SCREENING OF NOVEL IMIDAZOLE INCORPORATED HETEROCYCLIC 2-SUBSTITUTED ARYL-4-FLUORO PHENYL-5-(2-CHLOROPYRIDINYL)-1H-IMIDAZOLE DERIVATIVES

Rajesh Kumar Singh, Kaushal Chandrul*, Biswa Mohan Sahoo and Ravi Kant

Abstract

The valuable treatment of tuberculosis is difficult, due to the complicated or unusual structure and chemical composition of the mycobacterial cell wall. These complex properties of cell wall make many antibiotics and currently used drugs ineffective and hinder the entry of drugs in to the mycobacterium cells. Tuberculosis is still the one of the most crucial infectious disease worldwide. This paper describes the facile synthesis, characterization and in vitro anti-tubercular screening of novel imidazole incorporated heterocyclic 2-substituted aryl-4-fluoro phenyl-5-(2-Chloropyridinyl)-1H-imidazole derivatives which were synthesized by the reaction of 2-(2- chloropyridin-4-yl)-1-(4-fluorophenyl) ethanone [obtained by the reaction of ethyl -4- fluoro benzoate with 2-chloro-4-methylpyridine] with selenium dioxide in dioxane followed by cyclisation with substituted aryl(or hetero aryl)aldehyde in presence of acetic acid and ammonium acetate. The entire synthesized compounds were characterized by elemental analysis, 1H NMR and LCMS and also screened for their in- vitro antitubercular activity against Mycobacterium tuberculosis.

Keywords: Imidazole, selenium dioxide, ammonium acetate and anti tubercular activity.