吲哚衍生物的设计、合成及胰岛素增敏活性

Design, synthesis and insulin-sensitizing activity of indole derivatives

摘要: 目的设计合成具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，运用拼合设计原理，设计合成了10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。结果发现其中化合物4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。

Abstract: AimTo design and synthesize compounds with insulin-sensitizing activity. Methods Using association principle of drug design, ten title compounds were designed and synthesized on the basis of known compounds with insulin-sensitizing activity, and their insulin-sensitizing activity were evaluated on 3T3-L1 pre-adipocyte cells. ResultsOne of the synthesized compounds showed strong insulin-sensitizing activity in vitro. ConclusionThis compound may possess good sugar-lowering activity, and will be chosen for further hypoglycemic evaluation in vivo.