Selected arylpiperazines are capable of reversing multidrug resistance in Escherichia coli overexpressing RND efflux pumps.
Several arylpiperazines capable of reversing multidrug resistance (MDR) in Escherichia coli overexpressing acrAB and acrEF but not in pump-deficient mutant strains were identified. 1-(1-Naphthylmethyl)-piperazine, one of the more active compounds, enhanced susceptibility to fluoroquinolones and other agents and increased the intracellular concentration of levofloxacin and ethidium bromide, suggesting efflux pump inhibition as the mechanism of MDR reversal.
Bohnert
Jürgen A
JA
Center for Infectious Diseases and Travel Medicine, Department of Medicine, University Hospital, Freiburg, Germany.
Kern
Winfried V
WV
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D001426:Bacterial Proteins / Q000235:genetics; D002352:Carrier Proteins / Q000235:genetics; D024901:Drug Resistance, Multiple, Bacterial / Q000235:genetics* / Q000502:physiology*; D004926:Escherichia coli / Q000187:drug effects* / Q000235:genetics*; D064704:Levofloxacin; D008826:Microbial Sensitivity Tests; D009154:Mutation / Q000235:genetics; D015242:Ofloxacin / Q000494:pharmacology; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
C493251:AcrAB-TolC protein, Salmonella enterica; D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D002352:Carrier Proteins; D010879:Piperazines; D064704:Levofloxacin; D015242:Ofloxacin