Synthesis and Antimycobacterial Evaluation of N-(E)-heteroaromaticpyrazine-2-carbohydrazide Derivatives

Title: Synthesis and Antimycobacterial Evaluation of N-(E)-heteroaromaticpyrazine-2-carbohydrazide Derivatives

Volume: 7 Issue: 3

Author(s): C. H. S. Lima, M. G. M. O. Henriques, A. L. P. Candea, M. C. S. Lourenco, F. A. F. M. Bezerra, M. L. Ferreira, C. R. Kaiser and M. V. N. de Souza

Affiliation:

Keywords: Pyrazine, tuberculosis, drugs, N'-(E)-heteroaromatic-pyrazine-2-carbohydrazide, M. tuberculosis, Alamar Blue assay, minimum inhibitory concentration, macrophages, Mycobaterium bovis, Bacillus Calmette-Guerin

Abstract: A series of nine N'-(E)-heteroaromatic-pyrazine-2-carbohydrazide derivatives (5a-f and 6a-c) have been synthesized and evaluated against M. tuberculosis ATCC 27294 using the micro plate Alamar Blue assay (MABA), being the activities expressed as the minimum inhibitory concentration (MIC) in μg/ml. Compounds 5a and 5f exhibited potent activities (3.12 and 50μg/mL, respectively) when compared to the first line drug pyrazinamide (MIC > 100 μg/mL). Afterwards, these compounds were evaluated for their cell viabilities in non-infected and infected macrophages with Mycobaterium bovis Bacillus Calmette-Guerin (BCG) and 5f was not cytotoxic to host cells in the effective concentration to inhibit the growth of M. tuberculosis.

Cite this article as:

H. S. Lima C., G. M. O. Henriques M., L. P. Candea A., C. S. Lourenco M., A. F. M. Bezerra F., L. Ferreira M., R. Kaiser C. and V. N. de Souza M., Synthesis and Antimycobacterial Evaluation of N-(E)-heteroaromaticpyrazine-2-carbohydrazide Derivatives, Medicinal Chemistry 2011; 7 (3) . https://dx.doi.org/10.2174/157340611795564303