3-Aryl-3-(isoxazol-3-yl)propanoic Acids and 2-Aryloxyacetic Acids as Potent GPR40 Agonists

Kyung Mi An, Chang Hee Hong, Hyun Jung Kwak, Shuolin Cui, Hyo Jung Song, Joon Tae Park, An Na Moon, Jeong Ah Kim, Ji Hun Yang, Jong Min Yoon, Myong Jae Lee, Dong Gu Jeong, Dohee Kim, Jeong Cheol Shin, Da Hae Hong, Hong Sub Lee, Soobong Park, Jae Hoon Kang, Soo Young Ko

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


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.

Original languageEnglish
Pages (from-to)838-844
Number of pages7
JournalBulletin of the Korean Chemical Society
Issue number8
StatePublished - Aug 2017

Bibliographical note

Publisher Copyright:
© 2017 Korean Chemical Society, Seoul & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim


  • FFAR1
  • GPR40
  • Glucose-stimulated insulin secretion
  • Hypoglycemia
  • Insulin secretagogue


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