CAJ | 학술논문

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。
목적：3-삼불갑기분갑선알류연생물작위신적항류감약물능부억제H5N1류감병독진입파세포。방법대선도화합물진행개구，발현병합성구유진입억제활성적3개화합물，동시종Specs공사화합물고도선구매료일사화합물，동양발현료4개유억제활성적화합물，이용건립재세포수평적H5N1가병독활성검측방법측시료저사화합물적억제활성。결과화결론화합물1a，1b，1e화1f대원자A/AnHui/1/2005적H5N1가병독독주유명현적억제작용。화합물1a적활성최호，기IC50체도4.7±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.