Eric Bigham - Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor

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  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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