2. Academic Validation
  3. Discovery of a novel class of PPARdelta partial agonists

Discovery of a novel class of PPARdelta partial agonists

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5018-22. doi: 10.1016/j.bmcl.2008.08.011.
Barry G Shearer 1,  Hari S Patel,  Andrew N Billin,  James M Way,  Deborah A Winegar,  Millard H Lambert,  Robert X Xu,  Lisa M Leesnitzer,  Raymond V Merrihew,  Stephane Huet,  Timothy M Willson
Affiliations

Affiliation

  • 1 Department of Metabolic Chemistry, Metabolic Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA. barry.g.shearer@gsk.com
PMID: 18722772 DOI: 10.1016/j.bmcl.2008.08.011
Abstract

Anthranilic acid GW9371 was identified as a novel class of PPARdelta partial agonist through high-throughput screening. The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells.

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