Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a)

  • Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062.
P Douglas Boatman  1 ,  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
Affiliations
  • 1. Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. [email protected]
PMID: 20363624 DOI: 10.1016/j.bmcl.2010.03.062
Abstract

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.