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

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

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

Authors: An K.-M.; Hong C.-H.; Kwak H.-J.; Cui S.; Song H.-J.; Park J.-T.; Moon A.-N.; Kim J.-A.; Yang J.-H.; Yoon J.; Lee M.; Jeong D.-G.; Kim D.; Shin J.; Hong D.; Lee H.-S.; Park S.; Kang J.-H.; Ko S.Y.

Citation: Bulletin of the Korean Chemical Society vol. 38, no. 8, pp. 838 - 844

Keywords: FFAR1; Glucose-stimulated insulin secretion; GPR40; Hypoglycemia; Insulin secretagogue

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