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
Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/157340611795564303 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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