CAJ | 학술논문

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(3T3-11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PPARy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.
목적설계급합성신형분양이정산류항당뇨병화합물.방법관건보취채용친핵취대반응혹Mitsunobu축합반응파친지성편단화산성편단련접성일체,공합성료8개신목표물.용핵자공진、홍외、질보진행결구학인.결과체외이도소증민활성측시(3T3-11지방세포)결과현시,분별장라격렬동、필격렬동、목표물A화B가입이경존재이도소저항지방세포배양액중,용GOD-POD방법분석득도상청액포도당농도분별위5.942,6.339,6.226화6.512mmol·L-1.결론목표물A재이도소저항실험(3T3-L1지방세포)중항당뇨병활성개우시수PPARy격동제라격렬동화필격렬동지간,이목표물B적활성략저우필격렬동.
Aim To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds. Methods Eight 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. Results In vitro insulin-sensitizing activity (3T3-L1adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GODpioglitazone, compounds A and B were added to the insulin-resistant system. Conclusion In 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.