Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors
作者:Lan-hu Hao、Yan-ping Li、Wei-ying He、Hui-qiang Wang、Guang-zhi Shan、Jian-dong Jiang、Yu-huan Li、Zhuo-rong Li
DOI:10.1016/j.ejmech.2012.07.008
日期:2012.9
pharmaceutical investigation. In this work, substituted bisaryl amide compounds were found to be a new class of potential anti-influenza agents, and a series of substituted bisaryl amide compounds were synthesised and evaluated for their anti-influenza virus activities. The analysis of the results produced a preliminary structure–activity relationship study (SAR). Compounds 1a, 1g, 1h, 1j, 1l and 1n exhibited
每年,流感病毒都是致死和发病的持续原因,因此,它本身已成为药物研究的重要目标。在这项工作中,发现取代的双芳基酰胺化合物是一类潜在的抗流感药物,并且合成了一系列取代的双芳基酰胺化合物并评估了它们的抗流感病毒活性。结果分析产生了初步的结构-活性关系研究(SAR)。化合物1a,1g,1h,1j,1l和1n对甲型流感病毒(A /广东罗湖/ 219/2006,H1N1)表现出明显的抗病毒活性,抑制浓度为50%(IC50)用于病毒生长,范围从12.5到59.0μM。具体而言,化合物1j还具有抗耐奥司他韦的流感病毒(A / Jinnan / 15/2009)和B型流感病毒(B / Jifang / 13/97)的抗病毒活性,IC 50值分别为9.2μM和21.4μM。因此,化合物1j作为抗流感病毒的候选药物值得进一步研究。