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

作　　者：汤磊[1] 杨玉社[2] 嵇汝运[2] 

机构地区：[1]贵阳医学院药学院,贵州贵阳550004 [2]中国科学院上海生命科学研究院上海药物研究所国家新药研究重点实验室,上海201203

出　　处：《药学学报》2006年第3期225-229,共5页Acta Pharmaceutica Sinica

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。Aim To 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-LI pre-adipocyte cells. Results One of the synthesized compounds showed strong insulin-sensitizing activity in vitro. Conclusion This compound may possess good sugar-lowering activity, and will be chosen for further hypoglycemic evaluation in vivo.

关 键 词：胰岛素增敏活性 3T3-L1细胞 2型糖尿病 

分 类 号：R916.41[医药卫生—药学]