期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 22, 页码 9265-9274出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm401340p
关键词
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资金
- Spanish Ministerio de Ciencia e Innovacion [CTQ2011-22433]
- Generalitat de Catalunya [SCG-2009-294]
- Government of Andorra [ATCR2012/2013-00XX-AND]
- Geconcerteerde Onderzoeksacties [GOA/10/014]
- NIH [GMS6423]
We have synthesized and characterized a series of compounds containing the 3-azatetracyclo[5.2.1.15'8.01'sjundecane scaffold designed as analogues of amantadine, an inhibitor of the M2 proton channel of influenza A virus. Inhibition of the wild-type (WT) M2 channel and the amantadineresistant A/M2-S31N and A/M2-V27A mutant ion channels were measured in Xenopus oocytes using two-electrode voltage clamp (TEV) assays. Most of the novel compounds inhibited the WT ion channel in the submicromolar IC50. None of the compounds was found to inhibit the S31N mutant ion channel. The antiviral activity of three novel dual WT and A/M2-V27A channels inhibitors was confirmed by influenza virus yield assays.
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