2. Academic Validation
  3. Discovery of the first series of small molecule H5N1 entry inhibitors

Discovery of the first series of small molecule H5N1 entry inhibitors

  • J Med Chem. 2009 Dec 10;52(23):7368-71. doi: 10.1021/jm900275m.
Gaopeng Song 1,  Sen Yang,  Wei Zhang,  Yingli Cao,  Peng Wang,  Ning Ding,  Zaihong Zhang,  Ying Guo,  Yingxia Li
Affiliations

Affiliation

  • 1 Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
PMID: 19537689 DOI: 10.1021/jm900275m
Abstract

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 IC(50) of 7.22-9.25 microM. 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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