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  • 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.

Bioorganic & medicinal chemistry letters (2012-10-27)
Attila Sipos, Zsolt Török, Erzsébet Rőth, Attila Kiss-Szikszai, Gyula Batta, Ilona Bereczki, Zsolt Fejes, Anikó Borbás, Eszter Ostorházi, Ferenc Rozgonyi, Lieve Naesens, Pál Herczegh
RESUMEN

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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Sigma-Aldrich
Phthaldialdehyde, ≥97% (HPLC), powder (may contain lumps)
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Phthaldialdehyde Reagent, Solution Complete
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Phthaldialdehyde, suitable for HPLC fluorimetric detection of amino acids, ≥99% (HPLC), powder
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Phthaldialdehyde, for fluorescence, ≥99.0% (HPLC)
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Teicoplanin
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Phthaldialdehyde Reagent, Solution Incomplete