一类丙二酸衍生物的设计、合成及胰岛素增敏活性研究

 目的设计合成具备胰岛素增敏活性的系列化合物。方法以具备胰岛素增敏活性的化合物为基础,根据电子等排和同系物衍生化设计原理,设计合成了19个目标化合物,用3T3-L1前脂肪细胞对这些化合物进行了胰岛素增敏活性筛选。结果发现其中3个目标化合物在3T3-L1前脂肪细胞模型上表现出较强的胰岛素增敏活性。结论该化合物可能在体内具有降糖活性,拟选送进行体内降糖活性测试。

Study on Design, Synthesis and Insuli N-Sensitizing Activity of Malonic Acid Derivatives

OBJECTIVE To design and synthesize compounds with insulin-sensitizing activity. METHODS Using isosterisms and analogues generation principle of drug design, 19 title compounds were designed and synthesized on the basis of known compounds with insulin-sensitizing activity, and their insulin-sensitizing activity was evaluated in 3T3-L1 pre-adipocyte cells. RESULTS Three of the synthesized compounds showed strong insulin-sensitizing activity in vitro. CONCLUSION These compounds might possess good sugar-lowering activity, and are selected for further hypoglycemic evaluation in vivo.