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Exploring the size limit of templates for inhibitors of the M2 ion channel of influenza A virus.

Abstract：

:Amantadine inhibits the M2 proton channel of influenza A virus, yet its clinical use has been limited by the rapid emergence of amantadine-resistant virus strains. We have synthesized and characterized a series of polycyclic compounds designed as ring-contracted or ring-expanded analogues of amantadine. Inhibition of the wild-type (wt) M2 channel and the A/M2-S31N and A/M2-V27A mutant ion channels were measured in Xenopus oocytes using two-electrode voltage clamp (TEV) assays. Several bisnoradamantane and noradamantane derivatives inhibited the wt ion channel. The compounds bind to a primary site delineated by Val27, Ala30, and Ser31, though ring expansion restricts the positioning in the binding site. Only the smallest analogue 8 was found to inhibit the S31N mutant ion channel. The structure-activity relationship obtained by TEV assay was confirmed by plaque reduction assays with A/H3N2 influenza virus carrying wt M2 protein.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Duque MD,Ma C,Torres E,Wang J,Naesens L,Juárez-Jiménez J,Camps P,Luque FJ,DeGrado WF,Lamb RA,Pinto LH,Vázquez S

doi

10.1021/jm101334y

subject

Has Abstract

pub_date

2011-04-28 00:00:00

pages

2646-57

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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