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Bioorg Med Chem. 2008 Nov 15;16(22):9847-57. doi: 10.1016/j.bmc.2008.09.042. Epub 2008 Sep 19.

Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors.

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1
Bioorganic Chemistry Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu Tawi 180001, India.

Abstract

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.

PMID:
18848780
DOI:
10.1016/j.bmc.2008.09.042
[Indexed for MEDLINE]

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