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

Authors: Lima, C.H.S.; Henriques, M.G.M.O.; Candea, A.L.P.; Lourenço, M.C.S.; Bezerra, F.A.F.M.; Kaiser, C.R.; De Souza, M.V.N.


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.

Keywords: Pyrazine, tuberculosis, drugs, N’-(E)-heteroaromatic-pyrazine-2-carbohydrazide, M. tuberculosis, Alamar Blue assay, minimum inhibitory concentration, macrophages, Mycobaterium bovis, Bacillus Calmette-Guerin Document Type: Research Article DOI: http://dx.doi.org/10.2174/157340611795564303 Publication date: 1 de Janeiro de 2011

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