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Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands

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dc.contributor.authorPark, HG-
dc.contributor.authorChoi, JY-
dc.contributor.authorKim, MH-
dc.contributor.authorChoi, SH-
dc.contributor.authorPark, MK-
dc.contributor.authorLee, J-
dc.contributor.authorSuh, YG-
dc.contributor.authorCho, HW-
dc.contributor.authorOh, U-
dc.contributor.authorKim, HD-
dc.contributor.authorJoo, YH-
dc.contributor.authorShin, SS-
dc.contributor.authorKim, JK-
dc.contributor.authorJeong, YS-
dc.contributor.authorKoh, HJ-
dc.contributor.authorPark, YH-
dc.contributor.authorJew, SS-
dc.date.available2021-02-22T15:47:15Z-
dc.date.issued2005-02-
dc.identifier.issn0960-894X-
dc.identifier.issn1464-3405-
dc.identifier.urihttps://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/15539-
dc.description.abstractSeventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound I with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC50 = 31 nM) and N-(4-tet-t-butylphenyl)-4-(3-methylpyridine-2-yl)benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in Ca-45 (2+)-influx assay. (C) 2004 Elsevier Ltd. All rights reserved.-
dc.format.extent4-
dc.language영어-
dc.language.isoENG-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.titleBiarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands-
dc.typeArticle-
dc.publisher.location영국-
dc.identifier.doi10.1016/j.bmcl.2004.11.033-
dc.identifier.scopusid2-s2.0-19944433048-
dc.identifier.wosid000226935700028-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.15, no.3, pp 631 - 634-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.citation.volume15-
dc.citation.number3-
dc.citation.startPage631-
dc.citation.endPage634-
dc.type.docTypeArticle-
dc.description.isOpenAccessN-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.subject.keywordPlusCAPSAICIN-
dc.subject.keywordPlusTHIOUREAS-
dc.subject.keywordPlusLIGANDS-
dc.subject.keywordPlusANALOGS-
dc.subject.keywordPlusSUZUKI-
dc.subject.keywordPlusACIDS-
dc.subject.keywordAuthorvanilloid receptor-
dc.subject.keywordAuthorantagonist-
dc.subject.keywordAuthorstructure-activity relationship-
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