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

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.

Graphical abstractA series of novel functionalized 3-nitro-4-amino benzoic acids and 6-amino nicotinic acids and their agonist activity at GPR109b are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide