| Literature DB >> 21075629 |
Christopher A Luckhurst1, Marianne Ratcliffe, Linda Stein, Mark Furber, Sara Botterell, David Laughton, Wendy Tomlinson, Richard Weaver, Kamaldeep Chohan, Andrew Walding.
Abstract
We describe the discovery of small molecule benzazepine derivatives as agonists of human peroxisome proliferator-activated receptor δ (PPARδ) that displayed excellent selectivity over the PPARα and PPARγ subtypes. Compound 8 displayed good PK in the rat and efficacy in upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) mRNA in human primary myotubes, a biomarker for increased fatty acid oxidation.Entities:
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Year: 2010 PMID： 21075629 DOI： 10.1016/j.bmcl.2010.10.083
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823