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Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

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  • Payare L Sangwan
  • Jawahir L Koul
  • Surrinder Koul
  • Mallepally V Reddy
  • Thota, Niranjan
  • Inshad A Khan
  • Ashwani Kumar
  • Nitin P Kalia
  • Ghulam N Qazi

Based on our recent findings that piperine is a potent Staphylococcus aureus NorA efflux pump inhibitor (EPI), 38 piperine analogs were synthesized and bioevaluated for their EPI activity. Twenty-five of them were found active with potentiating activity equivalent or more than known EPIs like reserpine, carsonic acid and verapamil. The inhibitory mechanism of the compounds was confirmed by efflux inhibition assay using ethidium bromide as NorA substrate. The present communication describes the synthesis, bioevaluation and structure related activity of these efflux pump inhibitors.

OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind16
Udgave nummer22
Sider (fra-til)9847-57
Antal sider11
ISSN0968-0896
DOI
StatusUdgivet - 15 nov. 2008

ID: 189311674