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2013 , Vol. 33 >Issue 01: 125 - 131

DOI: https://doi.org/10.6023/cjoc201209017

研究论文

喹啉-多胺衍生物的合成及其活性评价

  • 罗稳 ,
  • 张震 ,
  • 王超杰
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  • 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

收稿日期: 2012-09-12

  修回日期: 2012-09-24

  网络出版日期: 2012-10-11

基金资助

国家自然科学基金重大研究计划培育(No. 90913001)资助项目.

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Synthesis and Biological Evaluation of Quioline-Polyamine Derivatives

  • Luo Wen ,
  • Zhang Zhen ,
  • Wang Chaojie
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  • a Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University, Kaifeng 475004;
    b Pharmaceutical College, Henan University, Kaifeng 475004

Received date: 2012-09-12

  Revised date: 2012-09-24

  Online published: 2012-10-11

Supported by

Project supported by the National Natural Science Foundation of China (No. 90913001).

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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 mmol/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

本文引用格式

罗稳 , 张震 , 王超杰 . 喹啉-多胺衍生物的合成及其活性评价[J]. 有机化学, 2013 , 33(01) : 125 -131 . DOI: 10.6023/cjoc201209017

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 PC12 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%.

Key words： quioline; polyamine; cell protection

参考文献

[1] Ku, B.-S. Neuropsychopharmacolagy, Peking University Medical Press, Peking, 2007, pp. 112～114 (in Chinese). (库宝善, 神经精神药理学, 北京大学医学出版社, 北京, 2007, pp. 112～114.)

[2] Cheng, Y.-X.; Du, G.-H. Chin. J. Med. Guide 2006, 8, 320 (in Chinese). (成银霞, 杜冠华, 中国医药导刊, 2006, 8, 320.)

[3] Xia, S.-W.; Mao, Y.-P.; Xue, Q.-Q.; Yu, L.-M. Chem. J. Chin. Univ. 2011, 32, 2415 (in Chinese). (夏树伟, 毛亚嫔, 薛倩倩, 于良民, 高等学校化学学报, 2011, 32, 2415.)

[4] Guo, Y.-B.; Liu, H.-B.; Xu, M. Chin. J. Org. Chem. 2012, 32, 413 (in Chinese). (郭永彪, 刘海波, 许明, 有机化学, 2012, 32, 413.)

[5] Perkins, M. N.; Stone, T. W. Brain Res. 1982, 247, 184.

[6] Stone, T. W. Eur. J. Med. Chem. 2000, 35, 179.

[7] Reddy, V. K.; Sarkar, A.; Valasinas, A.; Marton, L. J.; Basu. H. S.; Frydman, B. J. Med. Chem. 2001, 44, 404.

[8] Melchiorre, C.; Bolognesi, M. L.; Minarini, A.; Rosini, M.; Tumiatti, V. J. Med. Chem. 2010, 53, 5906.

[9] Jin, L.; Sugiyama, H.; Takigawa, M.; Katagiri, D.; Tomitori, H.; Nishimura, K.; Kaur, N.; Phanstiel, O.; Kitajima, M.; Takayama, H.; Okawara, T.; Williams, K.; Kashiwagi, K.; Igarashi, K. J. Pharmacol. Exp. Ther. 2007, 320, 47.

[10] Kashiwagi, K.; Williams, K.; Igarashi, K. Amino Acids 2007, 33, 299.

[11] Wang, C.-J.; Gan, Y.; Zhao, J.; Ji, B.-S. CN 101830848, 2010 [Chem. Abstr. 2010, 153, 480857].

[12] Mei, S.-N. M.S. Thesis, Zhejiang University, Hangzhou, 2010 (in Chinese). (梅苏宁, 硕士论文, 浙江大学, 杭州, 2010.)

[13] Cheng, P.-F.; Wang, Y.-X.; Zhao, J.; Wang, C.-J. Fine Chem. 2006, 23, 664 (in Chinese). (程鹏飞, 王玉霞, 赵瑾, 王超杰, 精细化工, 2010, 23, 664.)

[14] Mosmann, T. J. Immunol. Methods 1983, 65, 55.

[15] Masuko, T.; Namiki, R.; Nemoto, Y.; Miyake, M.; Kizawa, Y.; Suzuki, T.; Kashiwagi, K.; Igarashi, K.; Kusama, T. J. Pharmacol. Exp. Ther. 2009, 331, 522.

[16] Liu, M. M.S. Thesis, Henan University, Kaifeng, 2011 (in Chinese). (刘曼, 硕士论文, 河南大学, 开封, 2011.)

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