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Eur J Med Chem. 2011 Jan;46(1):52-7. doi: 10.1016/j.ejmech.2010.10.010. Epub 2010 Oct 16.

Discovery of highly potent agents against influenza A virus.

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Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, 190 Kai Yuan Avenue, Guangzhou Science Park, Guangzhou 510530, People's Republic of China.


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.

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