Synthesis and biological evaluation of N-alkylated 8-oxybenz [c] azepine derivatives as selective PPARδ agonists

…, M Furber, S Botterell, D Laughton, W Tomlinson…

文献索引：Luckhurst, Christopher A.; Ratcliffe, Marianne; Stein, Linda; Furber, Mark; Botterell, Sara; Laughton, David; Tomlinson, Wendy; Weaver, Richard; Chohan, Kamaldeep; Walding, Andrew Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 531 - 536

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被引用次数: 5

摘要

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.