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苯氧异丁酸类化合物的合成及其体外抗糖尿病活性(英文)
Authors
刘忠荣
曾庆乐
+6 more
李伯刚
王河清
王锋鹏
罗焕
赵玉芬
高小平
Publication date
12 February 2006
Publisher
Abstract
目的设计及合成新型苯氧异丁酸类抗糖尿病化合物。方法关键步骤采用亲核取代反应或M itsunobu缩合反应把亲脂性片段和酸性片段连接成一体,共合成了8个新目标物。用核磁共振、红外、质谱进行结构确认。结果体外胰岛素增敏活性测试(3T3-L1脂肪细胞)结果显示,分别将罗格列酮、吡格列酮、目标物A和B加入已经存在胰岛素抵抗脂肪细胞培养液中,用GOD-POD方法分析得到上清液葡萄糖浓度分别为5.942,6.339,6.226和6.512mmol.L-1。结论目标物A在胰岛素抵抗实验(3T3-L1脂肪细胞)中抗糖尿病活性介于市售PPARγ激动剂罗格列酮和吡格列酮之间,而目标物B的活性略低于吡格列酮
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Last time updated on 16/06/2016