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

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

Affiliation

  • 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.

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