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Bioorg Med Chem Lett. 2011 Jan 1;21(1):492-6. doi: 10.1016/j.bmcl.2010.10.117. Epub 2010 Oct 27.

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

Author information

1
Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, Leicestershire LE11 5RH, UK. chris.luckhurst@astrazeneca.com

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.

PMID:
21094606
DOI:
10.1016/j.bmcl.2010.10.117
[Indexed for MEDLINE]

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