Design and expeditious synthesis of organosilanes as potent antivirals targeting multidrug-resistant influenza A viruses

Yanmei Hu, Yuanxiang Wang, Fang Li, Chunlong Ma, Jun Wang

Research output: Contribution to journalArticle

13 Scopus citations

Abstract

The efficacy of current influenza vaccines and small molecule antiviral drugs is curtailed by the emerging of multidrug-resistant influenza viruses. As resistance to the only FDA-approved oral influenza antiviral, oseltamivir (Tamiflu), continues to rise, there is a clear need to develop the next-generation of antiviral drugs. Since more than 95% of current circulating influenza A viruses carry the S31N mutation in their M2 genes, the AM2-S31N mutant proton channel represents an attractive target for the development of broad-spectrum antivirals. In this study we report the design and synthesis of the first class of organosilanes that have potent antiviral activity against a panel of human clinical isolates of influenza A viruses, including viruses that are resistant to amantadine, oseltamivir, or both.

Original languageEnglish (US)
Pages (from-to)70-76
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume135
DOIs
StatePublished - 2017

Keywords

  • AM2 proton channel
  • AM2-S31N inhibitor
  • Antiviral
  • Influenza A virus
  • Organosilane

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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