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...

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Published inFrontiers in microbiology Vol. 7; p. 622
Main Authors Otręebska-Machaj, Ewa, Chevalier, Jacqueline, Handzlik, Jadwiga, Szymańska, Ewa, Schabikowski, Jakub, Boyer, Gérard, Bolla, Jean-Michel, Kieć-Kononowicz, Katarzyna, Pagès, Jean-Marie, Alibert, Sandrine
Format Journal Article
LanguageEnglish
Published Switzerland Frontiers Media 2016
Frontiers Media S.A
Subjects
AcrAB pump
antibiotics
Bacteriology
Chemical Sciences
Efflux pump blocker
Hydantoins
Life Sciences
Medicinal Chemistry
Microbiology
Microbiology and Parasitology
Multidrug resistance efflux pumps
AcrAB pump
multidrug resistance
efflux pump blocker
hydantoin
antibiotics
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Summary: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.
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Edited by: Ivan Rychlik, Veterinary Research Institute, Czech Republic
Reviewed by: Helen Zgurskaya, University of Oklahoma, USA; Alessandra Polissi, Università degli Studi di Milano-Bicocca, Italy; Kunihiko Nishino, The Institute of Scientific and Industrial Research, Osaka University, Japan
This article was submitted to Antimicrobials, Resistance and Chemotherapy, a section of the journal Frontiers in Microbiology
ISSN:1664-302X
1664-302X
DOI:10.3389/fmicb.2016.00622