一类丙二酸衍生物的设计、合成及胰岛素增敏活性研究  

Study on Design,Synthesis and Insuli N-Sensitizing Activity of Malonic Acid 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,贵阳550004 [2]中国科学院上海生命科学研究院,上海药物所国家新药研究重点实验室,上海201203

出　　处：《中国药学杂志》2007年第11期866-872,共7页Chinese Pharmaceutical Journal

摘　　要：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。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.

关 键 词：胰岛素增敏活性 3T3-L1细胞 2型糖尿病 

分 类 号：TQ467.32[化学工程—制药化工]