Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

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

doi:10.1016/j.bmc.2008.09.042

Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

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

Research output: Contribution to journal › Article › peer-review

106 Scopus citations

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.

Original language	English
Pages (from-to)	9847-9857
Number of pages	11
Journal	Bioorganic and Medicinal Chemistry
Volume	16
Issue number	22
DOIs	https://doi.org/10.1016/j.bmc.2008.09.042
State	Published - 15 Nov 2008
Externally published	Yes

Keywords

Ciprofloxacin
NorA efflux pumps inhibitor
Piperine analogs
Potentiator

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10.1016/j.bmc.2008.09.042

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title = "Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors",

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.",

keywords = "Ciprofloxacin, NorA efflux pumps inhibitor, Piperine analogs, Potentiator",

author = "Sangwan, \{Payare L.\} and Koul, \{Jawahir L.\} and Surrinder Koul and Reddy, \{Mallepally V.\} and Niranjan Thota and Khan, \{Inshad A.\} and Ashwani Kumar and Kalia, \{Nitin P.\} and Qazi, \{Ghulam N.\}",

year = "2008",

month = nov,

day = "15",

doi = "10.1016/j.bmc.2008.09.042",

language = "English",

volume = "16",

pages = "9847--9857",

journal = "Bioorganic and Medicinal Chemistry",

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TY - JOUR

T1 - Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

AU - Sangwan, Payare L.

AU - Koul, Jawahir L.

AU - Koul, Surrinder

AU - Reddy, Mallepally V.

AU - Thota, Niranjan

AU - Khan, Inshad A.

AU - Kumar, Ashwani

AU - Kalia, Nitin P.

AU - Qazi, Ghulam N.

PY - 2008/11/15

Y1 - 2008/11/15

N2 - 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.

AB - 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.

KW - Ciprofloxacin

KW - NorA efflux pumps inhibitor

KW - Piperine analogs

KW - Potentiator

UR - https://www.scopus.com/pages/publications/54849441199

U2 - 10.1016/j.bmc.2008.09.042

DO - 10.1016/j.bmc.2008.09.042

M3 - Article

C2 - 18848780

AN - SCOPUS:54849441199

SN - 0968-0896

VL - 16

SP - 9847

EP - 9857

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 22

ER -

Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors

Abstract

Keywords

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