GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
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.
Imbriglio
Jason E
JE
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA. jason_imbriglio@merck.com
Chang
Sookhee
S
Liang
Rui
R
Raghavan
Subharekha
S
Schmidt
Darby
D
Smenton
Abby
A
Tria
Scott
S
Schrader
Thomas O
TO
Jung
Jae-Kyu
JK
Esser
Craig
C
Holt
Tom G
TG
Wolff
Michael S
MS
Taggart
Andrew K P
AK
Cheng
Kang
K
Carballo-Jane
Ester
E
Waters
M Gerard
MG
Tata
James R
JR
Colletti
Steven L
SL
D000818:Animals; D005227:Fatty Acids / Q000378:metabolism; D006801:Humans; D051379:Mice; D009525:Niacin / Q000737:chemistry; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D011978:Receptors, Nicotinic / Q000378:metabolism
D005227:Fatty Acids; C530636:HCAR2 protein, human; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D009525:Niacin; C031280:pyrazole