Article
3-Azatetracyclo[5.2.1.1(5,8).0(1,5)]undecane derivatives: from wild-type inhibitors of the M2 ion channel of influenza A virus to derivatives with potent activity against the V27A mutant.
Journal of medicinal chemistry - 27 Nov 2013
Rey-Carrizo Matias, Torres Eva, Ma Chunlong, Barniol-Xicota Marta, Wang Jun, Wu Yibing, Naesens Lieve, DeGrado William F, Lamb Robert A, Pinto Lawrence H, Vázquez Santiago
Abstract excerpt
We have synthesized and characterized a series of compounds containing the 3-azatetracyclo[5.2.1.1(5,8).0(1,5)]undecane 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 amantadine-resistant A/M2-S31N and A/M2-V27A mutant ion channels were measured in Xenopus oocytes using two-electrode voltage clamp (TEV)...
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