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3‐Aryl‐3‐(isoxazol‐3‐yl)propanoic Acids and 2‐Aryloxyacetic Acids as Potent GPR40 Agonists
Author(s) -
An KyungMi,
Hong ChangHee,
Kwak HyunJung,
Cui Shuolin,
Song HyoJung,
Park JoonTae,
Moon AnNa,
Kim JeongAh,
Yang JiHun,
Yoon JongMin,
Lee MyongJae,
Jeong DongGu,
Kim Dohee,
Shin JeongCheol,
Hong DaHae,
Lee HongSub,
Park Soobong,
Kang JaeHoon,
Ko Soo Young
Publication year - 2017
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.11178
Subject(s) - free fatty acid receptor 1 , adme , agonist , pharmacophore , chemistry , pharmacology , partial agonist , propanoic acid , aryl , receptor , in vitro , biochemistry , stereochemistry , medicine , organic chemistry , alkyl
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.