4, 4-Dimethyl-1, 2, 3, 4-tetrahydroquinoline-based PPARα/γ agonists. Part I: Synthesis and pharmacological evaluation

…, N Hennuyer, B Staels, V Audinot-Bouchez…

Index: Parmenon, Cecile; Guillard, Jerome; Caignard, Daniel-Henri; Hennuyer, Nathalie; Staels, Bart; Audinot-Bouchez, Valerie; Boutin, Jean-Albert; Dacquet, Catherine; Ktorza, Alain; Viaud-Massuard, Marie-Claude Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 5 p. 1617 - 1622

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Citation Number: 30

Abstract

Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic β-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARα, PPARγ and PPARβ/(δ). We were interested in designing novel PPARγ selective agonists and/or dual PPARα/γ agonists. Based on the typical topology of ...