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  • Title: New macrocyclic amines showing activity as HIV entry inhibitors against wild type and multi-drug resistant viruses.
    Author: Rusconi S, Lo Cicero M, Viganò O, Sirianni F, Bulgheroni E, Ferramosca S, Bencini A, Bianchi A, Ruiz L, Cabrera C, Martinez-Picado J, Supuran CT, Galli M.
    Journal: Molecules; 2009 May 22; 14(5):1927-37. PubMed ID: 19471212.
    Abstract:
    Considering as a lead molecule the chemokine CXCR4 receptor antagonist AMD-3100, which shows significant anti-HIV activity in vitro and in vivo, we investigated a series of structurally related macrocyclic polyamines incorporating o,o'-phenanthroline or 2,2'-bipyridyl scaffolds as potential antiviral agents with lower toxicity and increased activity against both wild type X4-tropic and dual tropic HIV strains. The antiviral activity of these compounds was evaluated by susceptibility assays in PBMC (Peripheral Blood Mononuclear Cells) and compared to that of AMD-3100. The newly investigated compounds showed IC(50)s values in the low micromolar range and significantly inhibited the viral replication of wild type X4-tropic isolate and dual tropic strains. These macrocyclic polyamines constitute a promising class of HIV entry inhibitors.
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