Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo.
Boatman
P Douglas
PD
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. dboatman@arenapharm.com
Schrader
Thomas O
TO
Kasem
Michelle
M
Johnson
Benjamin R
BR
Skinner
Philip J
PJ
Jung
Jae-Kyu
JK
Xu
Jerry
J
Cherrier
Martin C
MC
Webb
Peter J
PJ
Semple
Graeme
G
Sage
Carleton R
CR
Knudsen
Jens
J
Chen
Ruoping
R
Taggart
Andrew K
AK
Carballo-Jane
Ester
E
Richman
Jeremy G
JG
D000818:Animals; D004285:Dogs; D000882:Haplorhini; D006801:Humans; D051379:Mice; D011720:Pyrazoles / Q000737:chemistry*; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D011978:Receptors, Nicotinic / Q000378:metabolism; D013777:Tetrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
C530636:HCAR2 protein, human; D011720:Pyrazoles; D043562:Receptors, G-Protein-Coupled; D011978:Receptors, Nicotinic; D013777:Tetrazoles; D014665:Vasodilator Agents; C031280:pyrazole