3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b

  • Bioorg Med Chem Lett. 2007 Dec 1;17(23):6619-22. doi: 10.1016/j.bmcl.2007.09.058.
Philip J Skinner  1 ,  Martin C Cherrier ,  Peter J Webb ,  Carleton R Sage ,  Huong T Dang ,  Cameron C Pride ,  Ruoping Chen ,  Susan Y Tamura ,  Jeremy G Richman ,  Daniel T Connolly ,  Graeme Semple
Affiliations
  • 1. Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. [email protected]
PMID: 17931863 DOI: 10.1016/j.bmcl.2007.09.058
Abstract

A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109A. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.

Products