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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

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

Volume 7 , Issue 3 , 2011

Page: [245 - 249] Pages: 5

DOI: 10.2174/157340611795564303

Price: $65


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.

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

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