2. Academic Validation
  3. Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists

Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. doi: 10.1016/j.bmcl.2010.10.117.
Christopher A Luckhurst 1,  Linda A Stein,  Mark Furber,  Nicola Webb,  Marianne J Ratcliffe,  Gary Allenby,  Sara Botterell,  Wendy Tomlinson,  Barrie Martin,  Andrew Walding
Affiliations

Affiliation

  • 1 Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, Leicestershire LE11 5RH, UK. chris.luckhurst@astrazeneca.com
PMID: 21094606 DOI: 10.1016/j.bmcl.2010.10.117
Abstract

Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human Peroxisome Proliferator-activated Receptor δ (PPARδ. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes.

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