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Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity
Multidrug resistant (MDR) bacteria are an increasing health problem with the shortage of new active antibiotic agents. Among effective mechanisms that contribute to the spread of MDR Gram-negative bacteria are drug efflux pumps that expel clinically important antibiotic classes out of the cell. Drug...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4853399/ https://www.ncbi.nlm.nih.gov/pubmed/27199950 http://dx.doi.org/10.3389/fmicb.2016.00622 |
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author | Otręebska-Machaj, Ewa Chevalier, Jacqueline Handzlik, Jadwiga Szymańska, Ewa Schabikowski, Jakub Boyer, Gérard Bolla, Jean-Michel Kieć-Kononowicz, Katarzyna Pagès, Jean-Marie Alibert, Sandrine |
author_facet | Otręebska-Machaj, Ewa Chevalier, Jacqueline Handzlik, Jadwiga Szymańska, Ewa Schabikowski, Jakub Boyer, Gérard Bolla, Jean-Michel Kieć-Kononowicz, Katarzyna Pagès, Jean-Marie Alibert, Sandrine |
author_sort | Otręebska-Machaj, Ewa |
collection | PubMed |
description | Multidrug resistant (MDR) bacteria are an increasing health problem with the shortage of new active antibiotic agents. Among effective mechanisms that contribute to the spread of MDR Gram-negative bacteria are drug efflux pumps that expel clinically important antibiotic classes out of the cell. Drug pumps are attractive targets to restore the susceptibility toward the expelled antibiotics by impairing their efflux activity. Arylhydantoin derivatives were investigated for their potentiation of activities of selected antibiotics described as efflux substrates in Enterobacter aerogenes expressing or not AcrAB pump. Several compounds increased the bacterial susceptibility toward nalidixic acid, chloramphenicol and sparfloxacin and were further pharmacomodulated to obtain a better activity against the AcrAB producing bacteria. |
format | Online Article Text |
id | pubmed-4853399 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-48533992016-05-19 Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity Otręebska-Machaj, Ewa Chevalier, Jacqueline Handzlik, Jadwiga Szymańska, Ewa Schabikowski, Jakub Boyer, Gérard Bolla, Jean-Michel Kieć-Kononowicz, Katarzyna Pagès, Jean-Marie Alibert, Sandrine Front Microbiol Microbiology Multidrug resistant (MDR) bacteria are an increasing health problem with the shortage of new active antibiotic agents. Among effective mechanisms that contribute to the spread of MDR Gram-negative bacteria are drug efflux pumps that expel clinically important antibiotic classes out of the cell. Drug pumps are attractive targets to restore the susceptibility toward the expelled antibiotics by impairing their efflux activity. Arylhydantoin derivatives were investigated for their potentiation of activities of selected antibiotics described as efflux substrates in Enterobacter aerogenes expressing or not AcrAB pump. Several compounds increased the bacterial susceptibility toward nalidixic acid, chloramphenicol and sparfloxacin and were further pharmacomodulated to obtain a better activity against the AcrAB producing bacteria. Frontiers Media S.A. 2016-05-03 /pmc/articles/PMC4853399/ /pubmed/27199950 http://dx.doi.org/10.3389/fmicb.2016.00622 Text en Copyright © 2016 Otrębska-Machaj, Chevalier, Handzlik, Szymańska, Schabikowski, Boyer, Bolla, Kieć-Kononowicz, Pagès and Alibert. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Microbiology Otręebska-Machaj, Ewa Chevalier, Jacqueline Handzlik, Jadwiga Szymańska, Ewa Schabikowski, Jakub Boyer, Gérard Bolla, Jean-Michel Kieć-Kononowicz, Katarzyna Pagès, Jean-Marie Alibert, Sandrine Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity |
title | Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity |
title_full | Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity |
title_fullStr | Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity |
title_full_unstemmed | Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity |
title_short | Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity |
title_sort | efflux pump blockers in gram-negative bacteria: the new generation of hydantoin based-modulators to improve antibiotic activity |
topic | Microbiology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4853399/ https://www.ncbi.nlm.nih.gov/pubmed/27199950 http://dx.doi.org/10.3389/fmicb.2016.00622 |
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