| Literature DB >> 17240142 |
Stephen C McKeown1, David F Corbett, Aaron S Goetz, Thomas R Littleton, Eric Bigham, Celia P Briscoe, Andrew J Peat, Steve P Watson, Deirdre M B Hickey.
Abstract
The discovery, synthesis and structure-activity relationship (SAR) of novel carboxylic acid agonists for GPR40 are described. Aryl propionic acid 1, identified from a high throughput screen, was selected for chemical exploration. Compound 2 was identified as our lead molecule through efficient solid phase combinatorial array chemistry and had an attractive in vitro and in vivo pharmacokinetic profile in rat. These ligands may prove useful in establishing a role for GPR40 in insulin regulation.Entities:
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Year: 2007 PMID： 17240142 DOI： 10.1016/j.bmcl.2006.12.084
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823