tetano
Editor, Senior Moderator
Eur J Med Chem. 2017 Apr 19;135:70-76. doi: 10.1016/j.ejmech.2017.04.038. [Epub ahead of print]
[h=1]Design and expeditious synthesis of organosilanes as potent antivirals targeting multidrug-resistant influenza A viruses.[/h] Hu Y[SUP]1[/SUP], Wang Y[SUP]1[/SUP], Li F[SUP]1[/SUP], Ma C[SUP]2[/SUP], Wang J[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] 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.
Copyright ? 2017 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] AM2 proton channel; AM2-S31N inhibitor; Antiviral; Influenza A virus; Organosilane
PMID: 28433777 DOI: 10.1016/j.ejmech.2017.04.038
[h=1]Design and expeditious synthesis of organosilanes as potent antivirals targeting multidrug-resistant influenza A viruses.[/h] Hu Y[SUP]1[/SUP], Wang Y[SUP]1[/SUP], Li F[SUP]1[/SUP], Ma C[SUP]2[/SUP], Wang J[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] 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.
Copyright ? 2017 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] AM2 proton channel; AM2-S31N inhibitor; Antiviral; Influenza A virus; Organosilane
PMID: 28433777 DOI: 10.1016/j.ejmech.2017.04.038