Zeng Qing-le, Wang He-qing, Luo Huan, Gao Xiao-ping, Liu Zhong-rong, Li Bo-gang, Wang Feng-peng, Zhao Yu-fen
Department of Chemistry and Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China.
Yao Xue Xue Bao. 2006 Feb;41(2):108-14.
To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds.
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.
In 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 x L(-1), respectively, when rosiglitazone, pioglitazone, compounds A and B were added to the insulin-resistant system.
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.
设计并合成新型苯氧基异丁酸类似物作为抗糖尿病化合物。
通过亲脂性部分与酸性部分结合，采用亲核取代或 Mitsunobu 缩合反应合成了 8 种新的目标化合物。这 8 种化合物通过 1H NMR、13C NMR、IR 和 MS 进行了确证。
体外胰岛素增敏活性（3T3-L1 脂肪细胞）表明，当将罗格列酮、吡格列酮、化合物 A 和 B 添加到胰岛素抵抗系统中时，用 GOD-POD 法检测的上清液培养葡萄糖浓度分别为 5.942、6.339、6.226 和 6.512 mmol·L(-1)。
目标化合物 A 的体外胰岛素增敏活性介于罗格列酮和吡格列酮之间，目标化合物 B 的活性略低于吡格列酮。
