Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists
DC Field | Value | Language |
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dc.contributor.author | Park, Eun Ju | - |
dc.contributor.author | Ahn, Young Gil | - |
dc.contributor.author | Jung, Seung Hyun | - |
dc.contributor.author | Bang, Hyo Jeong | - |
dc.contributor.author | Kim, Mira | - |
dc.contributor.author | Hong, Dong Jin | - |
dc.contributor.author | Kim, Jisook | - |
dc.contributor.author | Suh, Kwee Hyun | - |
dc.contributor.author | Kim, Young Jin | - |
dc.contributor.author | Kim, Doran | - |
dc.contributor.author | Kim, Eun-Yeong | - |
dc.contributor.author | Lee, Kiho | - |
dc.contributor.author | Min, Kyung Hoon | - |
dc.date.available | 2019-03-08T21:01:18Z | - |
dc.date.issued | 2014-09 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.issn | 1464-3405 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/11827 | - |
dc.description.abstract | Takeda 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.extent | 5 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.title | Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.bmcl.2014.07.026 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.17, pp 4271 - 4275 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000341339300039 | - |
dc.identifier.scopusid | 2-s2.0-84906933589 | - |
dc.citation.endPage | 4275 | - |
dc.citation.number | 17 | - |
dc.citation.startPage | 4271 | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 24 | - |
dc.type.docType | Article | - |
dc.publisher.location | 영국 | - |
dc.subject.keywordAuthor | TGR5 | - |
dc.subject.keywordAuthor | Pyrimidine | - |
dc.subject.keywordAuthor | Malonamide | - |
dc.subject.keywordAuthor | Agonist | - |
dc.subject.keywordAuthor | Bioisostere | - |
dc.subject.keywordPlus | BILE-ACID RECEPTOR | - |
dc.subject.keywordPlus | POTENT AGONISTS | - |
dc.subject.keywordPlus | GPBAR1 TGR5 | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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