GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles 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; Andrew K P Taggart; Kang Cheng; Ester Carballo-Jane; M Gerard Waters; James R Tata; Steven L Colletti

doi:10.1016/j.bmcl.2009.03.014

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2121-4. doi: 10.1016/j.bmcl.2009.03.014. Epub 2009 Mar 9.

Authors

Jason E Imbriglio¹, Sookhee Chang, Rui Liang, Subharekha Raghavan, Darby Schmidt, Abby Smenton, Scott Tria, Thomas O Schrader, Jae-Kyu Jung, Craig Esser, 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, United States. jason_imbriglio@merck.com

PMID: 19307116
DOI: 10.1016/j.bmcl.2009.03.014

Abstract

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

Publication types

Comparative Study

MeSH terms

Animals
Humans
Male
Mice
Mice, Inbred C57BL
Mice, Knockout
Nicotinic Agonists / chemistry
Nicotinic Agonists / pharmacology
Pyrazoles / chemistry*
Pyrazoles / pharmacology
Receptors, G-Protein-Coupled / agonists*
Receptors, G-Protein-Coupled / deficiency
Receptors, G-Protein-Coupled / physiology
Receptors, Nicotinic / deficiency
Receptors, Nicotinic / physiology
Tetrazoles / chemistry*
Tetrazoles / pharmacology
Vasodilation / drug effects
Vasodilation / physiology

Substances

HCAR2 protein, human
Nicotinic Agonists
Pyrazoles
Receptors, G-Protein-Coupled
Receptors, Nicotinic
Tetrazoles
pyrazole