南方医科大学学报

南方医科大学学报 ›› 2014, Vol. 34 ›› Issue (07): 961-.

• • 上一篇    下一篇

3-三氟甲基苯甲酰胺类衍生物对H5N1流感病毒进入靶细胞的抑制活性

朱志博，蔡云，杨洁，李湘潋，李润明，刘叔文   

  • 出版日期:2014-07-20 发布日期:2014-07-20

Inhibitory activities of 3-trifluoromethyl benzamide derivatives against the entry of
H5N1 influenza viruses

  • Online:2014-07-20 Published:2014-07-20

PDF

1173

摘要： 目的3-三氟甲基苯甲酰胺类衍生物作为新的抗流感药物能否抑制H5N1流感病毒进入靶细胞。方法对先导化合物进行
改构，发现并合成具有进入抑制活性的3个化合物，同时从Specs公司化合物库挑选购买了一些化合物，同样发现了4个有抑制
活性的化合物，利用建立在细胞水平的H5N1假病毒活性检测方法测试了这些化合物的抑制活性。结果和结论化合物1a，1b，
1e和1f对源自A/AnHui/1/2005的H5N1假病毒毒株有明显的抑制作用。化合物1a的活性最好，其IC50达到4.7±0.3 μmol/L。

Abstract: Objective To study the inhibitory activities of 3-trifluoromethyl benzamide derivatives against the entry of H5N1
influenza viruses. Methods The lead compound was structurally modified to obtain 3 compounds with inhibitory activities
against H5N1 influenza viruses. Specs compound librany was screened and 4 compounds were identified to have such
inhibitory activities. The inhibitory activities of these compounds were tested at a celluar level against H5N1 influenza viruses.
Results and Conclusion The compounds 1a, 1b, 1e and 1f showed signifcant inhibitory activities against the entry of A/AnHui/
1/2005 pseudovirus into the target cells with an IC50 value of 4.7±0.3 μmol/L.