Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor.

作者: Stephen C. McKeown , David F. Corbett , Aaron S. Goetz , Thomas R. Littleton , Eric Bigham

DOI: 10.1016/J.BMCL.2006.12.084

关键词:

摘要: The discovery, synthesis and structure-activity relationship (SAR) of novel carboxylic acid agonists for GPR40 are described. Aryl propionic 1, identified from a high throughput screen, was selected chemical exploration. Compound 2 as our lead molecule through efficient solid phase combinatorial array chemistry had an attractive in vitro vivo pharmacokinetic profile rat. These ligands may prove useful establishing role insulin regulation.

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