2,5-Disubstituted pyridines as potent GPR119 agonists.
A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR analysis, compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor.
GlaxoSmithKline, Research Triangle Park, NC 27709, USA. yulin.x.wu@gsk.com
Yulin
Y
Wu
Judith D
JD
Kuntz
Andrew J
AJ
Carpenter
Jing
J
Fang
Howard R
HR
Sauls
Daniel J
DJ
Gomez
Carina
C
Ammala
Yun
Y
Xu
Shane
S
Hart
Sarva
S
Tadepalli
D000818:Animals; D006207:Half-Life; D006801:Humans; D051379:Mice; D011725:Pyridines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D013329:Structure-Activity Relationship
C519854:GPR119 protein, human; D011725:Pyridines; D043562:Receptors, G-Protein-Coupled