2. Academic Validation
  3. Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities

Synthesis of isoindole and benzoisoindole derivatives of teicoplanin pseudoaglycon with remarkable antibacterial and antiviral activities

  • Bioorg Med Chem Lett. 2012 Dec 1;22(23):7092-6. doi: 10.1016/j.bmcl.2012.09.079.
Attila Sipos 1,  Zsolt Török,  Erzsébet Rőth,  Attila Kiss-Szikszai,  Gyula Batta,  Ilona Bereczki,  Zsolt Fejes,  Anikó Borbás,  Eszter Ostorházi,  Ferenc Rozgonyi,  Lieve Naesens,  Pál Herczegh
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, Medical and Health Science Center, University of Debrecen, Egyetem tér 1, H-4010 Debrecen, Hungary. sipos.attila@pharm.unideb.hu
PMID: 23099097 DOI: 10.1016/j.bmcl.2012.09.079
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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