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- Title
3-Aryl-3-(isoxazol-3-yl)propanoic Acids and 2-Aryloxyacetic Acids as Potent GPR40 Agonists.
- Authors
An, Kyung-Mi; Hong, Chang-Hee; Kwak, Hyun-Jung; Cui, Shuolin; Song, Hyo-Jung; Park, Joon-Tae; Moon, An-Na; Kim, Jeong-Ah; Yang, Ji-Hun; Yoon, JongMin; Lee, MyongJae; Jeong, Dong-Gu; Kim, Dohee; Shin, JeongCheol; Hong, DaHae; Lee, Hong-Sub; Park, Soobong; Kang, Jae-Hoon; Ko, Soo Young
- 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.
- Subjects
HYPOGLYCEMIA; PROPIONIC acid; TYPE 2 diabetes treatment; HYPOGLYCEMIC agents; CHEMICAL derivatives; DISEASE risk factors
- Publication
Bulletin of the Korean Chemical Society, 2017, Vol 38, Issue 8, p838
- ISSN
0253-2964
- Publication type
Article
- DOI
10.1002/bkcs.11178