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

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.

SUBMITTER: Hu Y

PROVIDER: S-EPMC5505654 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature

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

Hu Yanmei Y Wang Yuanxiang Y Li Fang F Ma Chunlong C Wang Jun J

European journal of medicinal chemistry 20170420

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 targe ...[more]

PMID: 28433777

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