Bioorganic and Medicinal Chemistry Letters p. 3609 - 3613 (2013)
Update date:2022-07-29
Topics: Optimization Novel Discovery Agonists Experimental terms Experimental Chemical terms Arylsulfonyl
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
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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(2013)