| Literature DB >> 17804224 |
Philip J Skinner1, Martin C Cherrier, Peter J Webb, Young-Jun Shin, Tawfik Gharbaoui, Andrew Lindstrom, Vu Hong, Susan Y Tamura, Huong T Dang, Cameron C Pride, Ruoping Chen, Jeremy G Richman, Daniel T Connolly, Graeme Semple.
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.Entities:
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Year: 2007 PMID： 17804224 DOI： 10.1016/j.bmcl.2007.07.101
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823