2,5-Disubstituted pyridines as potent GPR119 agonists

Yulin Wu; Judith D Kuntz; Andrew J Carpenter; Jing Fang; Howard R Sauls; Daniel J Gomez; Carina Ammala; Yun Xu; Shane Hart; Sarva Tadepalli

doi:10.1016/j.bmcl.2010.02.083

2,5-Disubstituted pyridines as potent GPR119 agonists

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2577-81. doi: 10.1016/j.bmcl.2010.02.083. Epub 2010 Feb 25.

Authors

Yulin Wu¹, Judith D Kuntz, Andrew J Carpenter, Jing Fang, Howard R Sauls, Daniel J Gomez, Carina Ammala, Yun Xu, Shane Hart, Sarva Tadepalli

Affiliation

¹ GlaxoSmithKline, Research Triangle Park, NC 27709, USA. [email protected]

PMID: 20227877
DOI: 10.1016/j.bmcl.2010.02.083

Abstract

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.

MeSH terms

Animals
Half-Life
Humans
Mice
Pyridines / chemistry
Pyridines / pharmacokinetics
Pyridines / pharmacology*
Receptors, G-Protein-Coupled / agonists*
Structure-Activity Relationship

Substances

GPR119 protein, human
Pyridines
Receptors, G-Protein-Coupled