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Cited 7 time in webofscience Cited 7 time in scopus
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Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists

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dc.contributor.authorPark, Eun Ju-
dc.contributor.authorAhn, Young Gil-
dc.contributor.authorJung, Seung Hyun-
dc.contributor.authorBang, Hyo Jeong-
dc.contributor.authorKim, Mira-
dc.contributor.authorHong, Dong Jin-
dc.contributor.authorKim, Jisook-
dc.contributor.authorSuh, Kwee Hyun-
dc.contributor.authorKim, Young Jin-
dc.contributor.authorKim, Doran-
dc.contributor.authorKim, Eun-Yeong-
dc.contributor.authorLee, Kiho-
dc.contributor.authorMin, Kyung Hoon-
dc.date.available2019-03-08T21:01:18Z-
dc.date.issued2014-09-
dc.identifier.issn0960-894X-
dc.identifier.issn1464-3405-
dc.identifier.urihttps://scholarworks.bwise.kr/cau/handle/2019.sw.cau/11827-
dc.description.abstractTakeda G-protein-coupled receptor 5 (TGR5) is a promising molecular target for metabolic diseases. A series of 4-(2,5-dichlorophenoxy)pyrimidine and cyclopropylmalonamide derivatives were synthesized as potent agonists of TGR5 based on a bioisosteric replacement strategy. Several compounds exhibited improved potency, compared to a reference compound with a pyridine scaffold. The pharmacokinetic profile of the representative compound 18 was considered moderate. (C) 2014 Elsevier Ltd. All rights reserved.-
dc.format.extent5-
dc.language영어-
dc.language.isoENG-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.titleDiscovery of novel pyrimidine and malonamide derivatives as TGR5 agonists-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmcl.2014.07.026-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.17, pp 4271 - 4275-
dc.description.isOpenAccessN-
dc.identifier.wosid000341339300039-
dc.identifier.scopusid2-s2.0-84906933589-
dc.citation.endPage4275-
dc.citation.number17-
dc.citation.startPage4271-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.citation.volume24-
dc.type.docTypeArticle-
dc.publisher.location영국-
dc.subject.keywordAuthorTGR5-
dc.subject.keywordAuthorPyrimidine-
dc.subject.keywordAuthorMalonamide-
dc.subject.keywordAuthorAgonist-
dc.subject.keywordAuthorBioisostere-
dc.subject.keywordPlusBILE-ACID RECEPTOR-
dc.subject.keywordPlusPOTENT AGONISTS-
dc.subject.keywordPlusGPBAR1 TGR5-
dc.subject.keywordPlusACTIVATION-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.description.journalRegisteredClasssci-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
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