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Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities |
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| Authors: | Attila Sipos Zsolt Török Erzsébet R?th Attila Kiss-Szikszai Gyula Batta Ilona Bereczki Zsolt Fejes Anikó Borbás Eszter Ostorházi Ferenc Rozgonyi Lieve Naesens Pál Herczegh |
| Institution: | 1. Department of Pharmaceutical Chemistry, Medical and Health Science Center, University of Debrecen, Egyetem tér 1, H-4010 Debrecen, Hungary;2. Department of Organic Chemistry, University of Debrecen, Egyetem tér 1, H-4010 Debrecen, Hungary;3. Microbiology Laboratory, Department of Dermatology, Venerology and Dermatooncology, Semmelweis University, Mária u. 41, H-1085 Budapest, Hungary;4. Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium |
| Abstract: | 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. |
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