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Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. Epub 2007 Aug 23.

Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.

Author information

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

Abstract

A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.

PMID:
17804224
DOI:
10.1016/j.bmcl.2007.07.101
[Indexed for MEDLINE]

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