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Synthesis and 11 beta hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group

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dc.contributor.authorKwon, Sung Wook-
dc.contributor.authorKang, Seung Kyu-
dc.contributor.authorLee, Jae Hong-
dc.contributor.authorBok, Joo Hwan-
dc.contributor.authorKim, Chi Hyun-
dc.contributor.authorRhee, Sang Dal-
dc.contributor.authorJung, Won Hoon-
dc.contributor.authorKim, Hee Youn-
dc.contributor.authorBae, Myung Ae-
dc.contributor.authorSong, Jin Sook-
dc.contributor.authorHa, Duck Chan-
dc.contributor.authorCheon, Hyae Gyoung-
dc.contributor.authorKim, Ki Young-
dc.contributor.authorAhn, Jin Hee-
dc.date.accessioned2021-09-07T16:25:33Z-
dc.date.available2021-09-07T16:25:33Z-
dc.date.created2021-06-14-
dc.date.issued2011-01-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://scholar.korea.ac.kr/handle/2021.sw.korea/113329-
dc.description.abstractA new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11 beta-hydroxysteroid dehydrogenase 1 (11 beta-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11 beta-HSD1, selectivity toward 11 beta-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11 beta-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice. (c) 2010 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.language.isoen-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subject11-BETA-HYDROXYSTEROID DEHYDROGENASE-
dc.subjectMETABOLIC SYNDROME-
dc.subjectVISCERAL OBESITY-
dc.subjectTYPE-1-
dc.subjectMICE-
dc.subjectHYPERGLYCEMIA-
dc.subjectDRUGS-
dc.titleSynthesis and 11 beta hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group-
dc.typeArticle-
dc.contributor.affiliatedAuthorHa, Duck Chan-
dc.identifier.doi10.1016/j.bmcl.2010.10.123-
dc.identifier.scopusid2-s2.0-78650509855-
dc.identifier.wosid000285544400089-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.21, no.1, pp.435 - 439-
dc.relation.isPartOfBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.citation.volume21-
dc.citation.number1-
dc.citation.startPage435-
dc.citation.endPage439-
dc.type.rimsART-
dc.type.docTypeArticle-
dc.description.journalClass1-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.subject.keywordPlus11-BETA-HYDROXYSTEROID DEHYDROGENASE-
dc.subject.keywordPlusMETABOLIC SYNDROME-
dc.subject.keywordPlusVISCERAL OBESITY-
dc.subject.keywordPlusTYPE-1-
dc.subject.keywordPlusMICE-
dc.subject.keywordPlusHYPERGLYCEMIA-
dc.subject.keywordPlusDRUGS-
dc.subject.keywordAuthorDiabetes-
dc.subject.keywordAuthor11beta-HSD1-
dc.subject.keywordAuthorThiazolidine-
dc.subject.keywordAuthorAdamantyl-
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