喹啉-多胺衍生物的合成及其活性评价有机化学.pdfVIP

DOI: 10.6023/cjoc201209017 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 喹啉-多胺衍生物的合成及其活性评价 罗 稳a 张 震a,b 王超杰*,a (a 河南大学天然药物与免疫工程重点实验室 开封 475004) (b 河南大学药学院 开封 475004) 摘要 设计合成了 13 个喹啉-多胺衍生物, 产物结构均经 1H NMR, ESI-MS 和元素分析确认. 采用噻唑蓝(MTT)法测试 了化合物对连二亚硫酸钠损伤肾上腺嗜铬细胞瘤(PC12)细胞的抑制作用, 结果表明所有目标化合物对 PC12 细胞损伤 均有较好的抑制作用, 部分化合物优于尼莫地平, 其中化合物 T6 和 T7 的活性最强, 10 μmol/L 浓度下损伤抑制率分别 为 28.04%和 27.58%. 关键词 喹啉; 多胺; 细胞保护 Synthesis and Biological Evaluation of Quioline-Polyamine Derivatives Luo, Wena Zhang, Zhena,b Wang, Chaojie*,a a ( Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University, Kaifeng 475004) b ( Pharmaceutical College, Henan University, Kaifeng 475004) Abstract Thirteen quioline-polyamine derivatives were designed and synthesized. The structures of these compounds were confirmed by 1H NMR, ESI-MS techniques and elemental analysis. The neurons protection activities of these compounds were evaluated by methyl thiazolyl tetrazolium (MTT) assay with sodium dithionite as an injury to adrenal pheochromocytoma (PC12) cells. The results showed that all the target compounds exhibited protection activity for PC 12 cells and some of them were better than nimodipine. The best compounds were T6 and T7 with protection rates of 28.04% and 27.58%. Keywords quioline; polyamine; cell protection 神经退行性疾病(Neu