Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos

We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC50 values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 µM), C. krusei (34 µM) and C. tropicalis (17 µM). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents.

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Main Authors: Cachiba,Thomas Haruo, Carvalho,Bruno Demartini, Carvalho,Diogo Teixeira, Cusinato,Marina, Prado,Clara Gavião, Dias,Amanda Latercia Tranches
Format: Digital revista
Language:Portuguese
Published: Sociedade Brasileira de Química 2012
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422012000800014
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spelling oai:scielo:S0100-404220120008000142012-09-05Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicosCachiba,Thomas HaruoCarvalho,Bruno DemartiniCarvalho,Diogo TeixeiraCusinato,MarinaPrado,Clara GaviãoDias,Amanda Latercia Tranches N-acylhydrazones antibacterial activity antifungal activity We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC50 values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 µM), C. krusei (34 µM) and C. tropicalis (17 µM). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaQuímica Nova v.35 n.8 20122012-01-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422012000800014pt10.1590/S0100-40422012000800014
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country Brasil
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region America del Sur
libraryname SciELO
language Portuguese
format Digital
author Cachiba,Thomas Haruo
Carvalho,Bruno Demartini
Carvalho,Diogo Teixeira
Cusinato,Marina
Prado,Clara Gavião
Dias,Amanda Latercia Tranches
spellingShingle Cachiba,Thomas Haruo
Carvalho,Bruno Demartini
Carvalho,Diogo Teixeira
Cusinato,Marina
Prado,Clara Gavião
Dias,Amanda Latercia Tranches
Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos
author_facet Cachiba,Thomas Haruo
Carvalho,Bruno Demartini
Carvalho,Diogo Teixeira
Cusinato,Marina
Prado,Clara Gavião
Dias,Amanda Latercia Tranches
author_sort Cachiba,Thomas Haruo
title Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos
title_short Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos
title_full Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos
title_fullStr Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos
title_full_unstemmed Síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados N-acilidrazônicos
title_sort síntese e avaliação preliminar da atividade antibacteriana e antifúngica de derivados n-acilidrazônicos
description We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC50 values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 µM), C. krusei (34 µM) and C. tropicalis (17 µM). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents.
publisher Sociedade Brasileira de Química
publishDate 2012
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422012000800014
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