Bereczki Ilona, Kicsák Máté, Dobray Laura, Borbás Anikó, Batta Gyula, Kéki Sándor, Nikodém Éva Nemes, Ostorházi Eszter, Rozgonyi Ferenc, Vanderlinden Evelien, Naesens Lieve, Herczegh Pál
Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary.
Department of Organic Chemistry, University of Debrecen, H-4032 Debrecen, Hungary.
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3251-4. doi: 10.1016/j.bmcl.2014.06.018. Epub 2014 Jun 16.
In order to obtain new, cluster-forming antibiotic compounds, teicoplanin pseudoaglycone derivatives containing two lipophilic n-octyl chains have been synthesized. The compounds proved to be poor antibacterials, but, surprisingly, they exhibited potent anti-influenza virus activity against influenza A strains. This antiviral action was related to inhibition of the binding interaction between the virus and the host cell. Related analogs bearing methyl substituents in lieu of the octyl chains, displayed no anti-influenza virus activity. Hence, an interaction between the active, dually n-octylated compounds and the lipid bilayer of the host cell can be postulated, to explain the observed inhibition of influenza virus attachment.
为了获得新的、能形成簇的抗生素化合物，已经合成了含有两条亲脂性正辛基链的替考拉宁假糖苷配基衍生物。这些化合物被证明是低效的抗菌剂，但令人惊讶的是，它们对甲型流感病毒株表现出强大的抗流感病毒活性。这种抗病毒作用与抑制病毒和宿主细胞之间的结合相互作用有关。带有甲基取代基以代替辛基链的相关类似物没有显示出抗流感病毒活性。因此，可以推测活性双正辛基化化合物与宿主细胞的脂质双层之间存在相互作用，以解释观察到的流感病毒附着抑制现象。
