Department of Pharmaceutical Chemistry, Medical and Health Science Center, University of Debrecen, Egyetem tér 1, H-4010 Debrecen, Hungary.
Bioorg Med Chem Lett. 2012 Dec 1;22(23):7092-6. doi: 10.1016/j.bmcl.2012.09.079. Epub 2012 Sep 29.
The primary amino function of teicoplanin pseudoaglycon has been transformed into arylthioisoindole or benzoisoindole and glycosylthioisoindole derivatives, in a reaction with o-phthalaldehyde or naphtalene-2,3-dicarbaldehyde and various thiols. All of the obtained semisynthetic antibiotics exhibited potent antibacterial activities against Gram-positive bacteria in the ng per ml concentration range. A few of them showed antiviral activity, in particular against influenza virus.
替考拉宁伪糖基的伯氨基与邻苯二醛或萘-2,3-二醛和各种硫醇反应，转化为芳基硫代异吲哚或苯并异吲哚和糖基硫代异吲哚衍生物。所有获得的半合成抗生素在纳克/毫升浓度范围内对革兰氏阳性菌表现出很强的抗菌活性。其中一些具有抗病毒活性，特别是抗流感病毒。
