Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.

Jian Ken Zhang,An-Rong Li,Ming Yu,Yingcai Wang,Jiang Zhu,Frank Kayser,Julio C Medina,Karen Siegler,Marion Conn,Bei Shan,Mark P Grillo,John Eksterowicz,Peter Coward,Jiwen Jim Liu

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

We describe the discovery of a series of arylsulfonyl 3-(pyridin-2-yloxy)anilines as GPR119 agonists derived from compound 1. Replacement of the three methyl groups in 1 with metabolically stable moieties led to the identification of compound 34, a potent and efficacious GPR119 agonist with improved pharmacokinetic (PK) properties.

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关键词

GPR119 agonist,Type 2 diabetes,Metabolic stability,SAR optimization

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