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

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

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±0.3μmol/L。

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±0.3μmol/L.