Aryl-3-(isoxazol-3-yl) propanoic Acids and 2-Aryloxyacetic Acids as Potent GPR40 Agonists
- 주제(키워드) GPR40 , FFAR1 , Insulin secretagogue , Glucose-stimulated insulin secretion , Hypoglycemia
- 등재 SCIE, SCOPUS
- 발행기관 WILEY-V C H VERLAG GMBH
- 발행년도 2017
- URI http://www.dcollection.net/handler/ewha/000000147234
- 본문언어 영어
- Published As http://dx.doi.org/10.1002/bkcs.11178
초록/요약
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.
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