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Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives

Two series of N’(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)R...

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Autores principales: Ferreira, Marcelle de L., Gonçalves, Raoni S.B., Cardoso, Laura N. de F., Kaiser, Carlos R., Candéa, Andre L.P., Henriques, Maria das Graças M. de O., Lourenço, Maria C.S., Bezerra, Flávio A.F.M., de Souza, Marcus V. N.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: TheScientificWorldJOURNAL 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5763922/
https://www.ncbi.nlm.nih.gov/pubmed/20623095
http://dx.doi.org/10.1100/tsw.2010.124
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author Ferreira, Marcelle de L.
Gonçalves, Raoni S.B.
Cardoso, Laura N. de F.
Kaiser, Carlos R.
Candéa, Andre L.P.
Henriques, Maria das Graças M. de O.
Lourenço, Maria C.S.
Bezerra, Flávio A.F.M.
de Souza, Marcus V. N.
author_facet Ferreira, Marcelle de L.
Gonçalves, Raoni S.B.
Cardoso, Laura N. de F.
Kaiser, Carlos R.
Candéa, Andre L.P.
Henriques, Maria das Graças M. de O.
Lourenço, Maria C.S.
Bezerra, Flávio A.F.M.
de Souza, Marcus V. N.
author_sort Ferreira, Marcelle de L.
collection PubMed
description Two series of N’(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds.
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spelling pubmed-57639222018-06-03 Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives Ferreira, Marcelle de L. Gonçalves, Raoni S.B. Cardoso, Laura N. de F. Kaiser, Carlos R. Candéa, Andre L.P. Henriques, Maria das Graças M. de O. Lourenço, Maria C.S. Bezerra, Flávio A.F.M. de Souza, Marcus V. N. ScientificWorldJournal Research Article Two series of N’(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds. TheScientificWorldJOURNAL 2010-07-07 /pmc/articles/PMC5763922/ /pubmed/20623095 http://dx.doi.org/10.1100/tsw.2010.124 Text en Copyright © 2010 Marcelle de L. Ferreira et al. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Ferreira, Marcelle de L.
Gonçalves, Raoni S.B.
Cardoso, Laura N. de F.
Kaiser, Carlos R.
Candéa, Andre L.P.
Henriques, Maria das Graças M. de O.
Lourenço, Maria C.S.
Bezerra, Flávio A.F.M.
de Souza, Marcus V. N.
Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
title Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
title_full Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
title_fullStr Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
title_full_unstemmed Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
title_short Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
title_sort synthesis and antitubercular activity of heteroaromatic isonicotinoyl and 7-chloro-4-quinolinyl hydrazone derivatives
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5763922/
https://www.ncbi.nlm.nih.gov/pubmed/20623095
http://dx.doi.org/10.1100/tsw.2010.124
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