Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins / genetics
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Carrier Proteins / genetics
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Drug Resistance, Multiple, Bacterial / genetics*
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Drug Resistance, Multiple, Bacterial / physiology*
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Escherichia coli / drug effects*
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Escherichia coli / genetics*
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Levofloxacin
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Microbial Sensitivity Tests
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Mutation / genetics
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Ofloxacin / pharmacology
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Piperazines / chemistry
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Piperazines / pharmacology*
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Structure-Activity Relationship
Substances
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AcrAB-TolC protein, Salmonella enterica
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Anti-Bacterial Agents
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Bacterial Proteins
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Carrier Proteins
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Piperazines
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Levofloxacin
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Ofloxacin