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Molecules 2009, 14(5), 1927-1937;

New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses

Dipartimento di Scienze Cliniche “Luigi Sacco”, Sezione di Malattie Infettive e Immunopatologia, Università degli Studi, Ospedale Luigi Sacco, via G.B. Grassi 74, 20157 Milano, Italy
Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Firenze), Italy
IrsiCaixa Foundation, University Hospital Germans Trias i Pujol, Badalona, Spain
Author to whom correspondence should be addressed.
Received: 2 April 2009 / Revised: 20 May 2009 / Accepted: 21 May 2009 / Published: 22 May 2009
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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 IC50s 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. View Full-Text
Keywords: HIV-1; co-receptors; CXCR4; macrocyclic polyamines HIV-1; co-receptors; CXCR4; macrocyclic polyamines

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Rusconi, S.; Cicero, M.L.; Viganò, O.; Sirianni, F.; Bulgheroni, E.; Ferramosca, S.; Bencini, A.; Bianchi, A.; Ruiz, L.; Cabrera, C.; Martinez-Picado, J.; Supuran, C.T.; Galli, M. New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses. Molecules 2009, 14, 1927-1937.

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