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Title: Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics
Authors: Balzarini, Jan ×
Pannecouque, Christophe
De Clercq, Erik
Pavlov, Andrey Y
Printsevskaya, Svetlana S
Miroshnikova, Olga V
Reznikova, Marina I
Preobrazhenskaya, Maria N #
Issue Date: Jun-2003
Series Title: Journal of Medicinal Chemistry vol:46 issue:13 pages:2755-2764
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.
URI: 
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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