有机化学 ›› 2015, Vol. 35 ›› Issue (6): 1335-1341.DOI: 10.6023/cjoc201501018 上一篇    下一篇

研究简报

嘧啶核苷-查尔酮杂化体的合成及其抗利什曼原虫活性研究

宰文静a, 蒋盼盼a, 张新迎a, Philippe M. Loiseaub, 郭胜海a, 范学森a   

  1. a 河南师范大学化学化工学院 河南省精细化学品绿色制造协同创新中心 绿色化学介质与反应省部共建教育部重点实验室 新乡453007;
    b 法国巴黎第十一大学药学院 沙特奈-马拉布里 F-92290 法国
  • 收稿日期:2015-01-14 修回日期:2015-02-11 发布日期:2015-02-12
  • 通讯作者: 张新迎, 范学森 E-mail:xinyingzhang@htu.cn;xuesen.fan@htu.cn
  • 基金资助:

    国家自然科学基金(Nos. 21172057, 21272058, 21202040)、河南省高校科技创新人才支持计划(No. 15HASTIT005)及河南省高校科技创新团队支持计划(No. 15IRTSTHN003)资助项目.

Synthesis and Antileishmanial Activity of Pyrimidine Nucleoside- Chalcone Hybrids

Zai Wenjinga, Jiang Panpana, Zhang Xinyinga, Loiseau Philippe M.b, Guo Shenghaia, Fan Xuesena   

  1. a Collaborative Innovation Centre of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007, China;
    b Chimioth閞apie Antiparasitaire, Facult?de Pharmacie, CNRS, UMR 8076 (BioCIS), Universit?Paris-Sud, 92290 Ch鈚enay-Malabry, France
  • Received:2015-01-14 Revised:2015-02-11 Published:2015-02-12
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21172057, 21272058, 21202040), the Program for Science and Technology Innovation Talents in Universities of Henan Province (No. 15HASTIT005), and the Program for Innovative Research Team in Science and Technology in University of Henan Province (No. 15IRTSTHN003).

以5-甲酰基嘧啶核苷为原料, 经与(取代)苯乙酮缩合, 得到了一系列含有嘧啶核苷和查尔酮两种优势结构单元的杂化体. 生物活性研究结果表明, 其中的一些杂化体具有显著的抗利什曼原虫活性, 从而为新药的开发提供了有价值的先导化合物和构效关系信息.

关键词: 嘧啶核苷, 查尔酮, 杂化体, 抗利什曼原虫活性

In this paper, a group of pyrimidine nucleoside-chalcone hybrids were conveniently prepared through condensing 5-formyl pyrimidine nucleosides with (substituted) acetophenones under the promotion of aqueous sodium hydroxide. The hybrid compounds were then evaluated as potential antileishmanial agents and some of them showed promisingly potent activities.

Key words: pyrimidine nucleosides, chalcones, hybrids, antileishmanial activity