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Updated: Feb 8, 2026

Methodology for the Study of Horizontal Gene Transfer in Staphylococcus aureus
Published on: March 10, 2017
Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position
Tommaso Felicetti1, Rolando Cannalire1, Maria Giulia Nizi1
1Department of Pharmaceutical Sciences, University of Perugia, via del Liceo 1, 06123, Perugia, Italy.
Abstract:
The alarming and rapid spread of antimicrobial resistance among bacteria represents a high risk for global health. Targeting factors involved in resistance to restore the activity of failing antibiotics is a promising strategy to overcome this urgent medical need. Efflux pump inhibitors are able to increase antibiotic concentrations in bacteria, thus they can be considered true antimicrobial resistance breakers. In this work, continuing our studies on inhibitors of the Staphylococcus aureus NorA pump, we designed, synthesized and biologically evaluated novel 2-phenylquinoline derivatives starting from our hits 1 and 2. Two of the synthesized compounds (6 and 7) bearing a C-6 benzyloxy group showed the best NorA inhibition activity, thereby providing an excellent starting point to direct future chemical optimizations.
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