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

作　　者：朱志博[1] 蔡云[1] 杨洁[1] 李湘潋[1] 李润明[1] 刘叔文[1] 

机构地区：[1]南方医科大学药学院,广东广州510515

出　　处：《南方医科大学学报》2014年第7期961-964,共4页Journal of Southern Medical University

基　　金：国家自然科学基金(81373263;U1301224);广东省自然科学基金(S2012040007938);高等学校博士学科点专项科研基金(新教师类)(20124433120023);广东省医学科研基金(B2011189)~~

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±0.3μmol/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.

关 键 词：H5N1禽流感病毒 流感病毒进入抑制剂 血凝素 苯甲酰胺 

分 类 号：R511.7[医药卫生—内科学]