3‐Aryl‐3‐(isoxazol‐3‐yl)propanoic Acids and 2‐Aryloxyacetic Acids as Potent GPR40 Agonists. (3rd August 2017)

• Record Type: Journal Article
• 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
• Is Part Of: Bulletin of the Korean Chemical Society. Volume 38:Number 8(2017)
• Page Start: 838
• Page End: 844
• Publication Date: 2017-08-03
• Subjects: GPR40 -- FFAR1 -- Insulin secretagogue -- Glucose‐stimulated insulin secretion -- Hypoglycemia; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/bkcs.11178
• Languages: English
• ISSNs: 0253-2964

Abstract

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 candidate2j as a novel GPR40 agonist. Abstract :