Modulation of PPAR subtype selectivity. Part 2: Transforming PPARα/γ dual agonist into α selective PPAR agonist through bioisosteric modification.

Bioorganic & Medicinal Chemistry Letters(2011)

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摘要
A novel series of oxime containing benzyl-1,3-dioxane-r-2-carboxylic acid derivatives are reported as selective PPARα agonists. Some of the test compounds exhibited good selectivity towards PPARα over PPARγ in vitro and the lead compound 6c showed excellent antihyperglycemic and antihyperlipidemic activity in vivo.
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关键词
Oxime,1,3-Dioxane-r-2-carboxylic acid,PPAR agonist,Type-2 diabetes,Metabolic disorders
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