Cargando…
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...
Autores principales: | , , , |
---|---|
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 |
_version_ | 1783498399123767296 |
---|---|
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. |
format | Online Article Text |
id | pubmed-7024281 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT cieslikwioleta antifungalstyryloquinolinesascandidaalbicanseffluxpumpinhibitorsstyryloquinolinesareabctransporterinhibitors AT szczepaniakjoanna antifungalstyryloquinolinesascandidaalbicanseffluxpumpinhibitorsstyryloquinolinesareabctransporterinhibitors AT krasowskaanna antifungalstyryloquinolinesascandidaalbicanseffluxpumpinhibitorsstyryloquinolinesareabctransporterinhibitors AT musiolrobert antifungalstyryloquinolinesascandidaalbicanseffluxpumpinhibitorsstyryloquinolinesareabctransporterinhibitors |