【文章名】4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPAR alpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPAR alpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations
[摘要]：Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a deficiency in pancreatic beta-cells. Since their discovery, three subtypes of peroxisome proliferator activated receptors have been identified, namely PPAR alpha, PPAR gamma and PPAR beta/(delta). In this study, we were interested in designing novel PPAR gamma selective agonists and/or dual PPAR alpha/gamma agonists. Based on the typical topology of synthetic PPAR agonists, we focused our design approach on using 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as a novel cyclic scaffold with oxime and acidic head group structural variations. (C) 2009 Elsevier Ltd. All rights reserved.
