Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidlyl peptidase IV (DPP-IV) inhibitors

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dc.contributor.authorAhn, Jin Heeko
dc.contributor.authorShin, Mi Sikko
dc.contributor.authorJun, Mi Aeko
dc.contributor.authorJung, Sun Hoko
dc.contributor.authorKang, Seung Kyuko
dc.contributor.authorKim, Kwang Rokko
dc.contributor.authorDal Rhee, Sangko
dc.contributor.authorKang, Nam Sookko
dc.contributor.authorKim, Sun Youngko
dc.contributor.authorSohn, Sang-Kwonko
dc.contributor.authorKim, Sung Gyuko
dc.contributor.authorJin, Mi Sunko
dc.contributor.authorLee, Jie-Ohko
dc.contributor.authorCheon, Hyae Gyeongko
dc.contributor.authorKim, Sung Sooko
dc.date.accessioned2009-09-11T06:01:01Z-
dc.date.available2009-09-11T06:01:01Z-
dc.date.created2012-02-06-
dc.date.created2012-02-06-
dc.date.issued2007-05-
dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.9, pp.2622 - 2628-
dc.identifier.issn0960-894X-
dc.identifier.urihttp://hdl.handle.net/10203/11147-
dc.description.abstractInhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of 0-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3 -amino-1-(2-benzoyl-1, 2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography. (c) 2007 Elsevier Ltd. All rights reserved.-
dc.description.sponsorshipThis research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program, the Ministry of Science and Technology, Korea. We thank the staff of the 4A and 6B beam lines of Pohang Accelerator Laboratory.en
dc.languageEnglish-
dc.language.isoen_USen
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectGLUCAGON-LIKE PEPTIDE-1-
dc.subjectTYPE-2 DIABETES-MELLITUS-
dc.subjectPYRAZOLIDINE DERIVATIVES-
dc.subjectGLUCOSE-TOLERANCE-
dc.subjectINSULIN-SECRETION-
dc.subjectPOTENT-
dc.subjectMICE-
dc.titleSynthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidlyl peptidase IV (DPP-IV) inhibitors-
dc.typeArticle-
dc.identifier.wosid000246087900046-
dc.identifier.scopusid2-s2.0-34047141757-
dc.type.rimsART-
dc.citation.volume17-
dc.citation.issue9-
dc.citation.beginningpage2622-
dc.citation.endingpage2628-
dc.citation.publicationnameBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.identifier.doi10.1016/j.bmcl.2007.01.111-
dc.embargo.liftdate9999-12-31-
dc.embargo.terms9999-12-31-
dc.contributor.localauthorLee, Jie-Oh-
dc.contributor.nonIdAuthorAhn, Jin Hee-
dc.contributor.nonIdAuthorShin, Mi Sik-
dc.contributor.nonIdAuthorJun, Mi Ae-
dc.contributor.nonIdAuthorJung, Sun Ho-
dc.contributor.nonIdAuthorKang, Seung Kyu-
dc.contributor.nonIdAuthorKim, Kwang Rok-
dc.contributor.nonIdAuthorDal Rhee, Sang-
dc.contributor.nonIdAuthorKang, Nam Sook-
dc.contributor.nonIdAuthorKim, Sun Young-
dc.contributor.nonIdAuthorSohn, Sang-Kwon-
dc.contributor.nonIdAuthorKim, Sung Gyu-
dc.contributor.nonIdAuthorJin, Mi Sun-
dc.contributor.nonIdAuthorCheon, Hyae Gyeong-
dc.contributor.nonIdAuthorKim, Sung Soo-
dc.type.journalArticleArticle-
dc.subject.keywordAuthorDPP-IV inhibitor-
dc.subject.keywordAuthordiabetes-
dc.subject.keywordAuthorcyclic hydrazine-
dc.subject.keywordPlusGLUCAGON-LIKE PEPTIDE-1-
dc.subject.keywordPlusTYPE-2 DIABETES-MELLITUS-
dc.subject.keywordPlusPYRAZOLIDINE DERIVATIVES-
dc.subject.keywordPlusGLUCOSE-TOLERANCE-
dc.subject.keywordPlusINSULIN-SECRETION-
dc.subject.keywordPlusPOTENT-
dc.subject.keywordPlusMICE-
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