Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities
Authors:
Sipos, Attila × Török, Zsolt Rőth, Erzsébet Kiss-Szikszai, Attila Batta, Gyula Bereczki, Ilona Fejes, Zsolt Borbás, Anikó Ostorházi, Eszter Rozgonyi, Ferenc Naesens, Lieve Herczegh, Pál #
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.
