Abstract

SYNTHESIS, DOCKING STUDIES OF QUINOLINE AMIDE DERIVATIVE AND EVALUATION FOR THEIR TUBERCULOSIS ACTIVITY

*T. Venkatachalam M.Pharm Ph.D, P. Suryamathi M.Pharm and Dr. N. Senthil Kumar M.Pharm Ph.D

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Abstract

In the present work, the design and synthesis a novel class of Quinoline amide fused heterocyclic derivatives have been carried out and substituted, and they were checked for docking scores against the Mycobacterium tuberculosis ligase enzyme. From that, ten best docked compounds are selected and synthesized and characterization of spectral data of the synthesized comopunds was obtained from IR, 1H NMR, 13C NMR, and mass spectroscopy,then the ten compounds are subjected to in-vitro Anti-Tuberculosis study by Luciferase Reporter phage (LRP) Assaymethod using H37RV strains of M. tuberculosis. Among the tested compounds, derivative P4 (92-98%) substituted with Quinoline amide moiety shows a significant activity against Mycobacterium tuberculosis ligase enzyme at different concentrations possesses Anti-Tuberculosis activity.

Keywords: Quinoline amide moiety, PyRx docking software, Mycobacterium tuberculosis ligase enzyme, Luciferase Reporter phage (LRP) Assaymethod,, Anti- Tuberculosis activity.