- Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Bioorganic & medicinal chemistry letters (2010-04-07)
P Douglas Boatman, Thomas O Schrader, Michelle Kasem, Benjamin R Johnson, Philip J Skinner, Jae-Kyu Jung, Jerry Xu, Martin C Cherrier, Peter J Webb, Graeme Semple, Carleton R Sage, Jens Knudsen, Ruoping Chen, Andrew K Taggart, Ester Carballo-Jane, Jeremy G Richman
PMID20363624
摘要
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.