Bioorganic & medicinal chemistry letters

Synthesis and evaluation of PSSRI-based inhibitors of Staphylococcus aureus multidrug efflux pumps

N German, GW Kaatz, RJ Kerns

Index: German, Nadezhda; Kaatz, Glenn W.; Kerns, Robert J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 4 p. 1368 - 1373

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Citation Number: 28

Abstract

Phenylpiperidine selective serotonin reuptake inhibitors (PSSRIs) block the function of selected multidrug efflux pumps of Staphylococcus aureus. In this study PSSRI-based piperidine derivatives were prepared, evaluated for inhibition of two multidrug resistance (MDR)-conferring efflux pump systems, and tested for potentiation of antimicrobial activity of antibacterial efflux pump substrates. It is demonstrated that the 4-phenyl moiety of PSSRI- ...