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Antibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group

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dc.contributor.authorSamosorn S.
dc.contributor.authorTanwirat B.
dc.contributor.authorMuhamad N.
dc.contributor.authorCasadei G.
dc.contributor.authorTomkiewicz D.
dc.contributor.authorLewis K.
dc.contributor.authorSuksamrarn A.
dc.contributor.authorPrammananan T.
dc.contributor.authorGornall K.C.
dc.contributor.authorBeck J.L.
dc.contributor.authorBremner J.B.
dc.date.accessioned2021-04-05T04:32:50Z
dc.date.available2021-04-05T04:32:50Z
dc.date.issued2009
dc.date.issuedBE2552
dc.description.abstractConjugation of the NorA substrate berberine and the NorA inhibitor 5-nitro-2-phenyl-1H-indole via a methylene ether linking group gave the 13-substituted berberine-NorA inhibitor hybrid, 3. A series of simpler arylmethyl ether hybrid structures were also synthesized. The hybrid 3 showed excellent antibacterial activity (MIC Staphylococcus aureus, 1.7 μM), which was over 382-fold more active than the parent antibacterial berberine, against this bacterium. This compound was also shown to block the NorA efflux pump in S. aureus. © 2009 Elsevier Ltd.
dc.format.mimetypeapplication/pdf
dc.identifier.citationBioorganic and Medicinal Chemistry. Vol 17, No.11 (2009), p.3866-3872
dc.identifier.doi10.1016/j.bmc.2009.04.028
dc.identifier.issn9680896
dc.identifier.other2-s2.0-65549100031
dc.identifier.urihttps://hdl.handle.net/20.500.14740/6519
dc.rights.holderScopus
dc.subject.other5 nitro 2 phenyl 1h indole
dc.subject.other9,10 dimethoxy 13 [2 (5 nitro 1h indol 2 yl)benzyloxy] 5,6 dihydrobenzo[g] 1,3 benzodioxolo[5,6 a]quinolizinium bromide
dc.subject.otherBerberine
dc.subject.otherBerberine 5 nitro 2 phenyl 1h indole conjugate
dc.subject.otherInf 55
dc.subject.otherNorA pump inhibitor
dc.subject.otherProtein inhibitor
dc.subject.otherUnclassified drug
dc.subject.otherAntibacterial activity
dc.subject.otherArticle
dc.subject.otherBacterial strain
dc.subject.otherControlled study
dc.subject.otherDrug conjugation
dc.subject.otherDrug potency
dc.subject.otherDrug structure
dc.subject.otherDrug synthesis
dc.subject.otherMinimum inhibitory concentration
dc.subject.otherNonhuman
dc.subject.otherStaphylococcus aureus
dc.subject.otherAnti-Bacterial Agents
dc.subject.otherBacterial Proteins
dc.subject.otherBerberine
dc.subject.otherEnterococcus faecalis
dc.subject.otherEther, Ethyl
dc.subject.otherIndoles
dc.subject.otherIntercalating Agents
dc.subject.otherMolecular Structure
dc.subject.otherMultidrug Resistance-Associated Proteins
dc.subject.otherStaphylococcus aureus
dc.subject.otherBacteria (microorganisms)
dc.subject.otherStaphylococcus aureus
dc.titleAntibacterial activity of berberine-NorA pump inhibitor hybrids with a methylene ether linking group
dc.typeArticle
dspace.entity.typePublication
swu.datasource.scopushttps://www.scopus.com/inward/record.uri?eid=2-s2.0-65549100031&doi=10.1016%2fj.bmc.2009.04.028&partnerID=40&md5=7d9a30a9bf253d6997e94fd82643d982

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