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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。
Objective To design and synthesize new phenoxyisobutyric acid antidiabetic compounds. Key steps of the method Nucleophilic substitution reaction or M itsunobu condensation reaction lipophilic fragments and acidic fragments into one, a total of eight new target synthesis. Structural verification was confirmed by nuclear magnetic resonance, infrared and mass spectrometry. Results The in vitro insulin sensitization activity test (3T3-L1 adipocytes) showed that rosiglitazone, pioglitazone, target A and B were added to the existing insulin resistance adipocyte medium and analyzed by GOD-POD method Serum glucose concentrations were 5.942, 6.339, 6.226 and 6.512 mmol.L-1, respectively. Conclusion The anti-diabetic activity of target A in insulin resistance experiments (3T3-L1 adipocytes) is between that of the commercially available PPARγ agonist rosiglitazone and pioglitazone, while that of target B is slightly lower than that of pioglitazone.