2. Academic Validation
  3. Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles

Chalcone inhibitors of the NorA efflux pump in Staphylococcus aureus whole cells and enriched everted membrane vesicles

  • Bioorg Med Chem. 2012 Jul 15;20(14):4514-21. doi: 10.1016/j.bmc.2012.05.025.
Jes Gitz Holler 1,  Hans-Christian Slotved,  Per Mølgaard,  Carl Erik Olsen,  Søren Brøgger Christensen
Affiliations

Affiliation

  • 1 University of Copenhagen, Faculty of Pharmaceutical Sciences, Department of Medicinal Chemistry, Denmark. [email protected]
PMID: 22682300 DOI: 10.1016/j.bmc.2012.05.025
Abstract

A library of 117 Chalcones was screened for efflux pump inhibitory (EPI) activity against NorA mediated ethidium bromide efflux. Five of the Chalcones (5-7, 9, and 10) were active and two Chalcones (9 and 10) were equipotent to reserpine with IC(50)-values of 9.0 and 7.7 μM, respectively. Twenty Chalcones were subsequently proved to be inhibitors of the NorA efflux pump in everted membrane vesicles. Compounds 5, 7, and 9 synergistically increased the effect of ciprofloxacin on Staphylococcus aureus. Our results suggest that Chalcones might be developed into drugs for overcoming multidrug resistance based on efflux transporters of Microorganisms.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-156753
    NorA Inhibitor