Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)

  • Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. doi: 10.1016/j.bmcl.2014.05.012.
Steven M Sparks  1 ,  Grace Chen  2 ,  Jon L Collins  3 ,  Dana Danger  3 ,  Steven T Dock  3 ,  Channa Jayawickreme  2 ,  Stephen Jenkinson  4 ,  Christopher Laudeman  4 ,  M Anthony Leesnitzer  2 ,  Xi Liang  3 ,  Patrick Maloney  4 ,  David C McCoy  4 ,  David Moncol  2 ,  Vincent Rash  2 ,  Thomas Rimele  2 ,  Padmaja Vulimiri  2 ,  James M Way  3 ,  Sean Ross  3
Affiliations
  • 1. Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States. Electronic address: [email protected].
  • 2. Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
  • 3. Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
  • 4. Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
PMID: 24881566 DOI: 10.1016/j.bmcl.2014.05.012
Abstract

The exploration of a diarylsulfonamide series of Free Fatty Acid Receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.

Keywords
FFA4; Free fatty acid receptor 4; Free fatty acid receptor 4 agonist; Free fatty acid receptor 4 antagonist; GPR120.
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