李家明 何 勇 周 鹏 徐云根 彭家志 盛日正. 阿魏酰胍丁胺类似物的设计、合成及Na+/H+交换器-1抑制活性J. 药学学报, 2011,46(8): 936-941.
引用本文: 李家明 何 勇 周 鹏 徐云根 彭家志 盛日正. 阿魏酰胍丁胺类似物的设计、合成及Na+/H+交换器-1抑制活性J. 药学学报, 2011,46(8): 936-941.
shu
LI Jia-Meng, He- Yong, Zhou- Feng, Xu-Yun-Gen, Bang-Jia-Zhi, Cheng-Ri-Zheng. Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analoguesJ. 药学学报, 2011,46(8): 936-941.
Citation: LI Jia-Meng, He- Yong, Zhou- Feng, Xu-Yun-Gen, Bang-Jia-Zhi, Cheng-Ri-Zheng. Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analoguesJ. 药学学报, 2011,46(8): 936-941.
shu

阿魏酰胍丁胺类似物的设计、合成及Na+/H+交换器-1抑制活性

Design, synthesis and Na+/H+ exchanger isoform-1 inhibitory activity of feruloylagmatine analogues

    摘要
  • 摘要:

    为了寻找新结构类型的Na+/H+交换器-1 (NHE-1) 抑制剂, 以阿魏酸、胍丁胺为先导化合物, 设计并合成了9个阿魏酰胍丁胺类似物。其结构经1H NMR、13C NMR和MS确证, 其中化合物5f～5i为新化合物。初步的药理实验结果表明, 部分目标化合物显示出较好的NHE抑制活性, 其中化合物5a、5b和6c对NHE-1的抑制活性明显优于阳性对照药卡立泊来德 (cariporide)。

     

    Abstract:

    In order to search for novel inhibitors of Na+/H+ exchanger isoform-1 (NHE-1), nine feruloylagmatine analogues were designed and synthesized from ferulic acid and agmatine.  The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR and mass spectra, among which compounds 5f−5i were novel compounds.  The results of preliminary pharmacological test showed that some of the compounds possessed strong NHE-1 inhibitory activity, among which compounds 5a, 5b and 6c were more potent than cariporide in NHE-1 inhibition.

     

    • 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