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Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

IR@IIIM: CSIR-Indian Institute of Integrative Medicine, Jammu

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Title Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors
 
Creator Sangwan, Payare L.
Koul, Jawahir L.
Koul, Surrinder
Reddy, Mallepally V.
Thota, Niranjan
Khan, Inshad A.
Kumar, Ashwani
Kalia, Nitin P.
Qazi, Ghulam N.
 
Subject Chemical Sciences
 
Description 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.
 
Date 2008
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://iiim.csircentral.net/309/1/10.1016j.bmc.2008.09.042.pdf
Sangwan, Payare L. and Koul, Jawahir L. and Koul, Surrinder and Reddy, Mallepally V. and Thota, Niranjan and Khan, Inshad A. and Kumar, Ashwani and Kalia, Nitin P. and Qazi, Ghulam N. (2008) Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors. Bioorganic & Medicinal Chemistry, 16 (22). pp. 9847-9857. ISSN 09680896
 
Relation http://dx.doi.org/10.1016/j.bmc.2008.09.042
http://iiim.csircentral.net/309/