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Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors

  作者 SONG GAOPENG; YANG SEN; ZHANG WEI; CAO YINGLI; WANG PENG; DING NING; ZHANG ZAIHONG; GUO YING; LI YINGXIA  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2009年52-23;  页码  7368-7371  
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[摘要]The occurrence of highly pathogenic avian influenza virus H5N1 highlights the urgent need for new classes of antiviral drugs. Inhibition of H5N1 entry into cells may be an effective strategy. We report the first three small molecule inhibitors saponins with 3-O-beta-chacotriosyl residue, which Showed potent inhibitory activity with IC50 of 7.22-9.25 mu M. The subsequent SAR studies showed the 3-O-beta-chacotriosyl residue was essential for the activity, and the aglycone structure also affected the activity.

 
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