122172-99-0Relevant academic research and scientific papers
Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics
Balzarini, Jan,Pannecouque, Christophe,De Clercq, Erik,Pavlov, Andrey Y.,Printsevskaya, Svetlana S.,Miroshnikova, Olga V.,Reznikova, Marina I.,Preobrazhenskaya, Maria N.
, p. 2755 - 2764 (2003)
A variety of semisynthetic derivatives of natural antibacterial glycopeptide antibiotics such as vancomycin, eremomycin, ristocetin A, teicoplanin A2-2, 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 μM) concentration range while not being cytostatic against human lymphocytic cells at 250 μM or higher. The mode of anti-HIV action of the antibiotic aglycon derivatives could be ascribed to inhibition of the viral entry process.
