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

…, G Allenby, S Botterell, W Tomlinson, B Martin…

Index: Luckhurst, Christopher A.; Stein, Linda A.; Furber, Mark; Webb, Nicola; Ratcliffe, Marianne J.; Allenby, Gary; Botterell, Sara; Tomlinson, Wendy; Martin, Barrie; Walding, Andrew Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 492 - 496

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Citation Number: 19

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.