Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, 190 Kai Yuan Avenue, Guangzhou Science Park, Guangzhou 510530, People's Republic of China.
Eur J Med Chem. 2011 Jan;46(1):52-7. doi: 10.1016/j.ejmech.2010.10.010. Epub 2010 Oct 16.
We previously reported several new M2 inhibitors as active as amantadine against influenza A virus and validated by three types of in vitro assays. Herein, we further modified one of the most potent hits in a viral inhibition assay and conducted structure-activity relationship studies on this scaffold. As a result, compound 8e was identified to be the most potent inhibitor against wild-type influenza A virus, being nearly 240-fold more active than amantadine.
我们之前报道了几种新型 M2 抑制剂，其对甲型流感病毒的活性与金刚烷胺相当，并通过三种体外检测方法得到了验证。在此基础上，我们进一步修饰了在病毒抑制检测中活性最高的化合物之一，并对该骨架进行了构效关系研究。结果表明，化合物 8e 是针对野生型流感病毒的最有效抑制剂，其活性比金刚烷胺高近 240 倍。
