Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors
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Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors. / Sangwan, Payare L; Koul, Jawahir L; Koul, Surrinder; Reddy, Mallepally V; Thota, Niranjan; Khan, Inshad A; Kumar, Ashwani; Kalia, Nitin P; Qazi, Ghulam N.
I: Bioorganic & Medicinal Chemistry, Bind 16, Nr. 22, 15.11.2008, s. 9847-57.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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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 - Alkaloids
KW - Anti-Bacterial Agents
KW - Bacterial Proteins
KW - Benzodioxoles
KW - Ciprofloxacin
KW - Enzyme Inhibitors
KW - Ethidium
KW - Microbial Sensitivity Tests
KW - Multidrug Resistance-Associated Proteins
KW - Nucleic Acid Synthesis Inhibitors
KW - Piperidines
KW - Polyunsaturated Alkamides
KW - Staphylococcus aureus
KW - Journal Article
U2 - 10.1016/j.bmc.2008.09.042
DO - 10.1016/j.bmc.2008.09.042
M3 - Journal article
C2 - 18848780
VL - 16
SP - 9847
EP - 9857
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
SN - 0968-0896
IS - 22
ER -
ID: 189311674