双喹啉-多胺缀合物的合成及生物活性测定

Synthesis and biological activitydetermination of bis-quinoline-polyamine conjugates

为了获得具有高活性的神经元保护药物,以1,3-丙二胺、1,4-丁二胺、1,6-己二胺等为原料,合成了4个新的双喹啉-多胺缀合物;利用核磁共振谱、质谱和元素分析确认了目标化合物的结构,同时评价了它们对神经元细胞的保护作用.结果表明,4个目标化合物对神经元细胞的保护作用均较差,说明多胺链并不能增强喹啉对神经元细胞的保护作用.

Four novel bis-quinoline-polyamine conjugates were synthesized with 1,3-propanedia-mine,1,4-bytanediamine and 1,6-hexanediamine as the starting materials in order to search drugs with high activity for neuroprotection.The structure of the as-synthesized products were confirmed by nuclear magnetic resonance spectrometry and mass spectrometry as well as ele-mental analysis,and their protection capabitities for neuron cell were evaluated.The prelimina-ry in vitro physiological activities against PC12 cell lines were also assessed.Results show that all the four as-synthesized target products exhibit poor protection capability for neuron cell, which indicates that the presence of the polyamine motif does not contribute to enhancing the protection capability of quinoline for neuron cell.