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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
- 고수영
- Issue Date
- 2017
- Journal Title
- Bulletin of the Korean Chemical Society
- ISSN
- 0253-2964
- Citation
- Bulletin of the Korean Chemical Society vol. 38, no. 8, pp. 861 - 868
- Keywords
- Glucose-stimulated insulin secretion; GPR40; Hypoglycemia; Insulin secretagogue
- Publisher
- Wiley Blackwell
- Indexed
- SCOPUS; KCI
- Document Type
- Article
- 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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