| Literature DB >> 26234904 |
Rieko Takano1, Masao Yoshida2, Masahiro Inoue3, Takeshi Honda4, Ryutaro Nakashima5, Koji Matsumoto5, Tatsuya Yano5, Tsuneaki Ogata6, Nobuaki Watanabe7, Masakazu Hirouchi7, Takako Kimura8, Narihiro Toda9.
Abstract
GPR40 agonists stimulate insulin secretion only under the presence of high glucose concentration. Based on this mechanism, GPR40 agonists are believed to be promising novel insulin secretagogues with low risk of hypoglycemia. The optimizations of 3-aryl-3-ethoxypropanoic acids were performed to improve in vitro activity. We discovered compound 29r (DS-1558), (3S)-3-ethoxy-3-(4-{[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]oxy}phenyl)propanoic acid, which was confirmed to have an enhancing effect on glucose-dependent insulin secretion after intravenous glucose injection in SD rats.Entities:
Keywords: Agonist; DS-1558; GPR40; Glucose-dependent; Insulin secretagogues
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Year: 2015 PMID： 26234904 DOI： 10.1016/j.bmc.2015.07.028
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641