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Bioorg Med Chem Lett. 2007 Dec 1;17(23):6619-22. Epub 2007 Sep 19.

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

Author information

1
Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. pskinner@arenapharm.com

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.

PMID:
17931863
DOI:
10.1016/j.bmcl.2007.09.058
[Indexed for MEDLINE]

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