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Discovery of 2,3-Dihydro-1H-indene Derivatives as Novel GPR40 Agonists

Title
Discovery of 2,3-Dihydro-1H-indene Derivatives as Novel GPR40 Agonists
Authors
An K.-M.Hong C.-H.Kwak H.-J.Cui S.Song H.-J.Park J.-T.Moon A.-N.Kim J.-A.Yang J.-H.Yoon J.Lee M.Jeong D.-G.Kim D.Lee D.-G.Shin J.Je I.-G.Lee H.-S.Park S.Kang J.-H.Ko S.Y.
Ewha Authors
고수영
SCOPUS Author ID
고수영scopus
Issue Date
2017
Journal Title
Bulletin of the Korean Chemical Society
ISSN
0253-2964JCR Link
Citation
vol. 38, no. 8, pp. 861 - 868
Keywords
Glucose-stimulated insulin secretionGPR40HypoglycemiaInsulin secretagogue
Publisher
Wiley Blackwell
Indexed
SCOPUS; KCI WOS scopus
Abstract
GPR40 (G protein-coupled receptor 40) has become an attractive target for insulin secretagogue via glucose-dependent mechanism with low risk of hypoglycemia. In order to overcome problems associated with previously developed GPR40 agonists, we recruited the core fragment 2,3-dihydro-1H-indene to GPR40 receptor binding pharmacophore with carboxylic acid moiety, and screened various amine analogs to finally discover several hit compounds displaying GPR40 agonistic activities. Through additional in vitro ADME, pharmacokinetics, and in vivo efficacy evaluations, compound 1e was demonstrated as a potent lead GPR40 agonist. © 2017 Korean Chemical Society, Seoul & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
DOI
10.1002/bkcs.11185
Appears in Collections:
자연과학대학 > 화학·나노과학전공 > Journal papers
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