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.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Anti-Bacterial Agents / chemical synthesis*
-
Anti-Bacterial Agents / chemistry
-
Anti-Bacterial Agents / pharmacology
-
Antiviral Agents / chemical synthesis*
-
Antiviral Agents / pharmacology
-
Antiviral Agents / toxicity
-
Cell Line
-
Cell Survival / drug effects
-
Drug Resistance, Viral / drug effects
-
Gram-Positive Bacteria / drug effects
-
Herpesvirus 1, Human / drug effects
-
Humans
-
Influenza A Virus, H1N1 Subtype / drug effects
-
Influenza A Virus, H3N2 Subtype / drug effects
-
Influenza B virus / drug effects
-
Isoindoles / chemical synthesis
-
Isoindoles / chemistry*
-
Microbial Sensitivity Tests
-
Teicoplanin / chemistry*
-
o-Phthalaldehyde / chemistry
Substances
-
Anti-Bacterial Agents
-
Antiviral Agents
-
Isoindoles
-
Teicoplanin
-
o-Phthalaldehyde