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Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors

Styrylquinolines are heterocyclic compounds that are known for their antifungal and antimicrobial activity. Metal complexation through hydroxyl groups has been claimed to be a plausible mechanism of action for these types of compounds. A series of novel structures with protected hydroxyl groups have...

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Autores principales: Cieslik, Wioleta, Szczepaniak, Joanna, Krasowska, Anna, Musiol, Robert
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7024281/
https://www.ncbi.nlm.nih.gov/pubmed/31952124
http://dx.doi.org/10.3390/molecules25020345
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author Cieslik, Wioleta
Szczepaniak, Joanna
Krasowska, Anna
Musiol, Robert
author_facet Cieslik, Wioleta
Szczepaniak, Joanna
Krasowska, Anna
Musiol, Robert
author_sort Cieslik, Wioleta
collection PubMed
description Styrylquinolines are heterocyclic compounds that are known for their antifungal and antimicrobial activity. Metal complexation through hydroxyl groups has been claimed to be a plausible mechanism of action for these types of compounds. A series of novel structures with protected hydroxyl groups have been designed and synthesized to verify the literature data. Their antifungal activity against wild-type Candida albicans strain and mutants with silenced efflux pumps activity has been determined. Combinations with fluconazole revealed synergistic interactions that were dependent on the substitution pattern. These results open a new route for designing active antifungal agents on a styrylquinoline scaffold.
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spelling pubmed-70242812020-03-11 Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors Cieslik, Wioleta Szczepaniak, Joanna Krasowska, Anna Musiol, Robert Molecules Article Styrylquinolines are heterocyclic compounds that are known for their antifungal and antimicrobial activity. Metal complexation through hydroxyl groups has been claimed to be a plausible mechanism of action for these types of compounds. A series of novel structures with protected hydroxyl groups have been designed and synthesized to verify the literature data. Their antifungal activity against wild-type Candida albicans strain and mutants with silenced efflux pumps activity has been determined. Combinations with fluconazole revealed synergistic interactions that were dependent on the substitution pattern. These results open a new route for designing active antifungal agents on a styrylquinoline scaffold. MDPI 2020-01-15 /pmc/articles/PMC7024281/ /pubmed/31952124 http://dx.doi.org/10.3390/molecules25020345 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Cieslik, Wioleta
Szczepaniak, Joanna
Krasowska, Anna
Musiol, Robert
Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors
title Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors
title_full Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors
title_fullStr Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors
title_full_unstemmed Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors
title_short Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors
title_sort antifungal styryloquinolines as candida albicans efflux pump inhibitors: styryloquinolines are abc transporter inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7024281/
https://www.ncbi.nlm.nih.gov/pubmed/31952124
http://dx.doi.org/10.3390/molecules25020345
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