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

…, Y Wang, J Zhu, F Kayser, JC Medina, K Siegler…

文献索引：Zhang, Jian; Li, An-Rong; Yu, Ming; Wang, Yingcai; Zhu, Jiang; Kayser, Frank; Medina, Julio C.; Siegler, Karen; Conn, Marion; Shan, Bei; Grillo, Mark P.; Eksterowicz, John; Coward, Peter; Liu, Jiwen Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 12 p. 3609 - 3613

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被引用次数: 9

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.