钟朝斌, 朱学军, 刘忠荣, 高小平, 王学超. PPARγ激动剂的设计、合成及其胰岛素增敏活性J. 药学学报, 2005, 40(2): 136-140.
引用本文: 钟朝斌, 朱学军, 刘忠荣, 高小平, 王学超. PPARγ激动剂的设计、合成及其胰岛素增敏活性J. 药学学报, 2005, 40(2): 136-140.
shu
ZHONG Chao-bin, ZHU Xue-jun, LIU Zhong-rong, GAO Xiao-ping, WANG Xue-chao. Design, synthesis and insulin-sensitizing activity of some peroxisome proliferator-activated γ agonistsJ. Acta Pharmaceutica Sinica, 2005, 40(2): 136-140.
Citation: ZHONG Chao-bin, ZHU Xue-jun, LIU Zhong-rong, GAO Xiao-ping, WANG Xue-chao. Design, synthesis and insulin-sensitizing activity of some peroxisome proliferator-activated γ agonistsJ. Acta Pharmaceutica Sinica, 2005, 40(2): 136-140.
shu

PPARγ激动剂的设计、合成及其胰岛素增敏活性

Design, synthesis and insulin-sensitizing activity of some peroxisome proliferator-activated γ agonists

    摘要
  • 摘要: 目的寻找新的高效、低毒的PPARγ激动剂。方法以JTT-501和JTT-20993为先导化合物，设计并合成新的丙二酸类和异恶唑类化合物，并测定其胰岛素增敏活性。结果共合成了8个新化合物,用核磁共振、质谱和红外光谱进行结构确证，并用胰岛素筛选模型初步评价了这些化合物的胰岛素增敏活性。化合物1A-4A显示胰岛素增敏活性,其中化合物1A和3A有较强活性。结论化合物1A和3A值得进一步评价。

     

    Abstract: AimTo find new peroxisome proliferator-activated γ agonists with high activity and low toxicity. MethodsBased on JTT-501 and JTT-20993, new isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds were designed and synthesized. Their insulin-sensitizing activities were evaluated. ResultsEight new compounds were obtained. The structures of synthesized compounds were characterized by NMR, MS and IR. Four compounds (1A-4A) showed insulin-sensitizing activities. ConclusionCompounds (1A and 3A) showed excellent insulin-sensitizing activities and should be worth further investigation.

     

    • HTML全文
    • 参考文献(0)
    • 相关文章
    • 施引文献
  • 资源附件(0)

/

返回文章
返回