Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms

We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values < 15 µM. The 6-amide derivatives displayed the highest fungici...

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Autores principales: Delattin, Nicolas, Bardiot, Dorothée, Marchand, Arnaud, Chaltin, Patrick, De Brucker, Katrijn, Cammue, Bruno P. A., Thevissen, Karin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268363/
https://www.ncbi.nlm.nih.gov/pubmed/23079495
http://dx.doi.org/10.3390/molecules171012243
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author Delattin, Nicolas
Bardiot, Dorothée
Marchand, Arnaud
Chaltin, Patrick
De Brucker, Katrijn
Cammue, Bruno P. A.
Thevissen, Karin
author_facet Delattin, Nicolas
Bardiot, Dorothée
Marchand, Arnaud
Chaltin, Patrick
De Brucker, Katrijn
Cammue, Bruno P. A.
Thevissen, Karin
author_sort Delattin, Nicolas
collection PubMed
description We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values < 15 µM. The 6-amide derivatives displayed the highest fungicidal activity against C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values of 6.25–12.5 µM. Compounds 1 and 5 of this series displayed fungicidal activity against the emerging pathogen Candida glabrata(MFC < 50 µM). The 6-amide derivatives 1, 2, 5, and 6 and the 6-urea derivatives 10, 12, 13 and 15 could also eradicate C. albicans biofilms. We found that the 6-urea derivatives 10, 13, and 15 induced accumulation of endogenous reactive oxygen species in Candida albicans biofilms.
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spelling pubmed-62683632018-12-12 Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms Delattin, Nicolas Bardiot, Dorothée Marchand, Arnaud Chaltin, Patrick De Brucker, Katrijn Cammue, Bruno P. A. Thevissen, Karin Molecules Article We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values < 15 µM. The 6-amide derivatives displayed the highest fungicidal activity against C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values of 6.25–12.5 µM. Compounds 1 and 5 of this series displayed fungicidal activity against the emerging pathogen Candida glabrata(MFC < 50 µM). The 6-amide derivatives 1, 2, 5, and 6 and the 6-urea derivatives 10, 12, 13 and 15 could also eradicate C. albicans biofilms. We found that the 6-urea derivatives 10, 13, and 15 induced accumulation of endogenous reactive oxygen species in Candida albicans biofilms. MDPI 2012-10-18 /pmc/articles/PMC6268363/ /pubmed/23079495 http://dx.doi.org/10.3390/molecules171012243 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Delattin, Nicolas
Bardiot, Dorothée
Marchand, Arnaud
Chaltin, Patrick
De Brucker, Katrijn
Cammue, Bruno P. A.
Thevissen, Karin
Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
title Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
title_full Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
title_fullStr Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
title_full_unstemmed Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
title_short Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
title_sort identification of fungicidal 2,6-disubstituted quinolines with activity against candida biofilms
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268363/
https://www.ncbi.nlm.nih.gov/pubmed/23079495
http://dx.doi.org/10.3390/molecules171012243
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