有机化学 ›› 2018, Vol. 38 ›› Issue (5): 1147-1154.DOI: 10.6023/cjoc201712017 上一篇    下一篇

研究论文

吗啉核苷类似物及其磺胺衍生物的合成及初步抗牛病毒性腹泻病毒(BVDV)活性研究

华迎春a,b, 贺斌a,b, 秦之焱a,b, 王松a,b, 刘慧萍a,b, 刘丰五a,b   

  1. a 郑州大学药学院 郑州 450001;
    b 新药创制与安全性评价河南省协同创新中心 郑州 450001
  • 收稿日期:2017-12-08 修回日期:2018-01-10 发布日期:2018-01-26
  • 通讯作者: 刘丰五,E-mail:fwliu@zzu.edu.cn E-mail:fwliu@zzu.edu.cn
  • 基金资助:

    国家自然科学基金(No.21372207)资助项目.

Synthesis and Preliminary Anti-bovine Viral Diarrhea Virus (BVDV) Activity Evaluation of Morpholine Nucleoside Analogues and Their Sulfonamide Derivatives

Hua Yingchuna,b, He Bina,b, Qin Zhiyana,b, Wang Songa,b, Liu Huipinga,b, Liu Fengwua,b   

  1. a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b Collaborative Innovation Center of Henan New Drug Research and Safety Evaluation, Zhengzhou 450001
  • Received:2017-12-08 Revised:2018-01-10 Published:2018-01-26
  • Contact: 10.6023/cjoc201712017 E-mail:fwliu@zzu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21372207).

以核糖核苷为原料,通过糖环的结构转化合成了系列吗啉核苷类似物,再与磺胺类药物的母核偶联得到吗啉核苷磺胺衍生物.所得化合物均经HRMS、1H NMR和13C NMR谱分析确证.以牛病毒性腹泻病毒(BVDV)感染的牛肾细胞为模型对目标化合物抗病毒活性进行筛选,结果显示此类化合物无明显抗病毒活性.

关键词: 核苷类似物, 吗啉核苷, 磺胺类衍生物, 抗BVDV活性

A series of morpholine nucleoside analogues were synthesized starting from ribonucleosides, and then the morpholine nucleoside sulfonamide derivatives were obtained by treated with N-acetylsulfanilyl chloride. The obtained compounds were confirmed by HRMS, 1H NMR and 13C NMR spectral analysis. The bovine kidney cells infected with bovine viral diarrhea virus (BVDV) were used as models to screen the antiviral activity of the target compounds. But the results did not show desired potent antiviral activity.

Key words: nucleoside analogue, morpholine nucleoside, sulfonamides derivative, anti-BVDV activity