曾庆乐, 王河清, 罗焕, 高小平, 刘忠荣, 李伯刚, 王锋鹏, 赵玉芬. 苯氧异丁酸类化合物的合成及其体外抗糖尿病活性J. 药学学报, 2006, 41(2): 108-114.
引用本文: 曾庆乐, 王河清, 罗焕, 高小平, 刘忠荣, 李伯刚, 王锋鹏, 赵玉芬. 苯氧异丁酸类化合物的合成及其体外抗糖尿病活性J. 药学学报, 2006, 41(2): 108-114.
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ZENG Qing-le, WANG He-qing, LUO Huan, GAO Xiao-ping, LIU Zhong-rong, LI Bo-gang, WANG Feng-peng, ZHAO Yu-fen. Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitroJ. Acta Pharmaceutica Sinica, 2006, 41(2): 108-114.
Citation: ZENG Qing-le, WANG He-qing, LUO Huan, GAO Xiao-ping, LIU Zhong-rong, LI Bo-gang, WANG Feng-peng, ZHAO Yu-fen. Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitroJ. Acta Pharmaceutica Sinica, 2006, 41(2): 108-114.
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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

Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro

    摘要
  • 摘要: 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Mitsunobu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6.512 mmol·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。

     

    Abstract: AimTo design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds. MethodsEight new target compounds were synthesized by combination of lipophilic moieties and acidic moiety with nucleophilic replacement or Mitsunobu condensation. The eight compounds were confirmed by 1H NMR, 13C NMR, IR and MS. ResultsIn vitro insulin-sensitizing activity (3T3-L1 adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GOD-POD assay were 5.942, 6.339, 6.226 and 6.512 mmol·L-1, respectively, when rosiglitazone, pioglitazone, compounds A and B were added to the insulin-resistant system. ConclusionIn vitro insulin-sensitizing activity of target compound A is in between that of rosiglitazone and pioglitazone, and activity of target compound B is slightly less than that of pioglitazone.

     

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