New pyridoquinoline derivatives as potential inhibitors of the fluoroquinolone efflux pump in resistant Enterobacter aerogenes strains
| Autor: | Annie Eyraud, Siham Atifi, Abdallah Mahamoud, Jean-Marie Pagès, Jacqueline Chevalier, Jacques Barbe |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Membrane permeability
medicine.drug_class Microbial Sensitivity Tests Enterobacter aerogenes Microbiology Structure-Activity Relationship Anti-Infective Agents Bacterial Proteins Drug Discovery Drug Resistance Bacterial medicine Norfloxacin Antibacterial agent biology Chemistry Escherichia coli Proteins Quinolone biology.organism_classification Enterobacteriaceae Drug Resistance Multiple Multiple drug resistance DNA-Binding Proteins Biochemistry Quinolines Molecular Medicine Thermodynamics Efflux Drug Antagonism medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 44(23) |
| ISSN: | 0022-2623 |
| Popis: | Enterobacter aerogenes, one of the most frequently isolated nosocomial pathogens in France, is exhibiting increasing multidrug resistance mechanisms associated with a change in membrane permeability. For drugs of the quinolone family, mutations in the target and active efflux play a prominent role in the resistance. We report here the effect of several pyridoquinoline derivatives that restore a noticeable fluoroquinolone accumulation to resistant strains that overexpress the MarA activator. Studies of the energy-dependent quinolone efflux indicate that the most efficient derivatives tested probably inhibit the resistance process by acting as substrate competitors on the pump extruding intracellular norfloxacin. |
| Databáze: | OpenAIRE |
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