Publication Details (including relevant citation information):
By McKeown, Stephen C.; Corbett, David F.; Goetz, Aaron S.; Littleton, Thomas R.; Bigham, Eric; Briscoe, Celia P.; Peat, Andrew J.; Watson, Steve P.; Hickey, Deirdre M. B.
From Bioorganic & Medicinal Chemistry Letters (2007), 17(6), 1584-1589.
The discovery, synthesis and structure-activity relationship (SAR) of novel carboxylic acid agonists for GPR40 are described. Aryl propionic acid I, identified from a high throughput screen, was selected for chem. exploration. Compd. II was identified as our lead mol. through efficient solid phase combinatorial array chem. 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.
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