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3-Aryl-3-(isoxazol-3-yl)propanoic Acids and 2-Aryloxyacetic Acids as Potent GPR40 Agonists

Title
3-Aryl-3-(isoxazol-3-yl)propanoic Acids and 2-Aryloxyacetic Acids as Potent 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.Shin J.Hong D.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. 838 - 844
Keywords
FFAR1Glucose-stimulated insulin secretionGPR40HypoglycemiaInsulin secretagogue
Publisher
Wiley Blackwell
Indexed
SCOPUS; KCI WOS scopus
Abstract
GPR40 is one of the most prominent targets for the treatment of type 2 diabetes (T2DM), and has its role in insulin secretion via blood-glucose-dependent manner with a minimum risk of hypoglycemia. In order to discover novel antidiabetics bearing these benefits, we screened various derivatives with two distinct pharmacophores. Both series displayed potent agonistic activities for GPR40 in vitro functional assay. Through additional ADME and in vivo efficacy evaluations, we identified the potent hit candidate 2j as a novel GPR40 agonist. © 2017 Korean Chemical Society, Seoul & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
DOI
10.1002/bkcs.11178
Appears in Collections:
자연과학대학 > 화학·나노과학전공 > Journal papers
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