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.
Affiliations
- 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.