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  • Title: Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics.
    Author: Balzarini J, Pannecouque C, De Clercq E, Pavlov AY, Printsevskaya SS, Miroshnikova OV, Reznikova MI, Preobrazhenskaya MN.
    Journal: J Med Chem; 2003 Jun 19; 46(13):2755-64. PubMed ID: 12801238.
    Abstract:
    A variety of semisynthetic derivatives of natural antibacterial glycopeptide antibiotics such as vancomycin, eremomycin, ristocetin A, teicoplanin A(2)-2, DA-40926, their aglycons, and also the products of their partial degradation with a destroyed or modified peptide core show marked anti-retroviral activity in cell culture. In particular, aglycon antibiotic derivatives containing various substituents of a preferably hydrophobic nature displayed activity against human immunodeficiency virus type 1 (HIV-1), HIV-2, and Moloney murine sarcoma virus at a 50% inhibitory concentration in the lower micromolar (1-5 microM) concentration range while not being cytostatic against human lymphocytic cells at 250 microM or higher. The mode of anti-HIV action of the antibiotic aglycon derivatives could be ascribed to inhibition of the viral entry process.
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