Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c] pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists
The discovery and optimization of novel N-(3-(1,3-dioxo-2,3-dihydro-1H- pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamide GPR119 agonists is described. Modification of the pyridylphthalimide motif of the molecule with R1 =-Me and R2 =-iPr substituents, incorporated with a 6-fluoro substitution on the central phenyl ring offered a potent and metabolically stable tool compound 22.
Yu, Ming,Zhang, Jian,Wang, Yingcai,Zhu, Jiang,Kayser, Frank,Medina, Julio C.,Siegler, Karen,Conn, Marion,Shan, Bei,Grillo, Mark P.,Coward, Peter,Liu, Jiwen
p. 156 - 160
(2014/01/17)
Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists
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.
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
p. 3609 - 3613
(2013/07/25)
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