STUDY OF NOVEL SUBSTITUTED 1, 2, 4-TRIAZOLES AS POTENT ANTI-TUBERCULAR AGENTS

Konda Reddy Girija, K. Abdul Gafoor, K. Hemalatha and V. N. Azger Dusthackeer

ABSTRACT

A series of Mannich based substituted 1,2,4-triazoles were synthesized by condensation of 1,5 diphenyl 1,2- dihydro -3H- 1,2,4-triazoles-3-thione with different primary amines. The structures of the synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR and Mass spectral analysis. The synthesized compounds were docked against the target enzyme Pantothenate synthetase using Autodock 1.5.4 version to predict the interaction between the atoms of the synthesized compounds and the amino acid residues of the target enzyme. The compound 3c, 3d, 3e, 3f and 3g showed a significant binding affinity against the target enzyme and these compounds were evaluated for their Anti-tubercular activity using LRP (Luciferase Reporter Phage) Method. All the tested compounds showed 97-98% of inhibition at the concentration of 500 μg/ml.

Keywords: Triazoles, Pantothenate synthetase, Anti-tubercular, Luciferace Reporter Phage.