GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

Jason E Imbriglio; Sookhee Chang; Rui Liang; Subharekha Raghavan; Darby Schmidt; Abby Smenton; Scott Tria; Thomas O Schrader; Jae-Kyu Jung; Craig Esser; Tom G Holt; Michael S Wolff; Andrew K P Taggart; Kang Cheng; Ester Carballo-Jane; M Gerard Waters; James R Tata; Steven L Colletti

doi:10.1016/j.bmcl.2010.06.041

GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4. doi: 10.1016/j.bmcl.2010.06.041. Epub 2010 Jun 10.

Authors

Jason E Imbriglio¹, Sookhee Chang, Rui Liang, Subharekha Raghavan, Darby Schmidt, Abby Smenton, Scott Tria, Thomas O Schrader, Jae-Kyu Jung, Craig Esser, Tom G Holt, Michael S Wolff, Andrew K P Taggart, Kang Cheng, Ester Carballo-Jane, M Gerard Waters, James R Tata, Steven L Colletti

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA. jason_imbriglio@merck.com

PMID: 20615702
DOI: 10.1016/j.bmcl.2010.06.041

Abstract

5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.

MeSH terms

Animals
Fatty Acids / metabolism
Humans
Mice
Niacin / chemistry
Pyrazoles / chemical synthesis
Pyrazoles / chemistry*
Pyrazoles / pharmacokinetics
Receptors, G-Protein-Coupled / agonists*
Receptors, G-Protein-Coupled / metabolism
Receptors, Nicotinic / metabolism

Substances

Fatty Acids
HCAR2 protein, human
Pyrazoles
Receptors, G-Protein-Coupled
Receptors, Nicotinic
Niacin
pyrazole