2. Academic Validation
  3. Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists

Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists

  • Bioorg Med Chem Lett. 2014 Jul 1;24(13):2949-53. doi: 10.1016/j.bmcl.2014.04.065.
Rieko Takano 1,  Masao Yoshida 1,  Masahiro Inoue 1,  Takeshi Honda 1,  Ryutaro Nakashima 1,  Koji Matsumoto 1,  Tatsuya Yano 1,  Tsuneaki Ogata 1,  Nobuaki Watanabe 1,  Narihiro Toda 2
Affiliations

Affiliations

  • 1 R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • 2 R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. Electronic address: toda.narihiro.jw@daiichisankyo.co.jp.
PMID: 24835985 DOI: 10.1016/j.bmcl.2014.04.065
Abstract

The G protein-coupled receptor 40 (GPR40) mediates enhancement of glucose-stimulated Insulin secretion in pancreatic β cells. The GPR40 agonist has been attracting attention as a novel Insulin secretagogue with glucose dependency for the treatment of type 2 diabetes. The optimization study of compound 1 led to a potent and bioavailable GPR40 agonist 24, which showed Insulin secretion and glucose lowering effects in rat OGTT. Compound 24 is a potential lead compound for a novel Insulin secretagogue with a low risk of hypoglycemia.

Keywords

Agonist; Diabetes; GPR40; Glucose lowering; Insulin secretagogue.

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