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

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

Index: 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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Citation Number: 5

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.

Design, synthesis, and evaluation of fused heterocyclic anal...

[Shah, Unmesh; Lankin, Claire M.; Boyle, Craig D.; Chackalamannil, Samuel; Greenlee, William J.; Neustadt, Bernard R.; Cohen-Williams, Mary E.; Higgins, Guy A.; Ng, Kwokei; Varty, Geoffrey B.; Zhang, Hongtao; Lachowicz, Jean E. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 4204 - 4209]

A new facile synthetic route to [11 C] GSK189254, a selectiv...

[Wang, Min; Gao, Mingzhang; Steele, Brandon L.; Glick-Wilson, Barbara E.; Brown-Proctor, Clive; Shekhar, Anantha; Hutchins, Gary D.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4713 - 4718]