Molecules 2009, 14(5), 1927-1937; doi:10.3390/molecules14051927
Article

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

Received: 2 April 2009; in revised form: 20 May 2009 / Accepted: 21 May 2009 / Published: 22 May 2009
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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 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.
Keywords: HIV-1; co-receptors; CXCR4; macrocyclic polyamines
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MDPI and ACS Style

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.

AMA Style

Rusconi S, Cicero ML, Viganò O, Sirianni F, Bulgheroni E, Ferramosca S, Bencini A, Bianchi A, Ruiz L, Cabrera C, Martinez-Picado J, Supuran CT, Galli M. New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses. Molecules. 2009; 14(5):1927-1937.

Chicago/Turabian Style

Rusconi, Stefano; Cicero, Mirko Lo; Viganò, Ottavia; Sirianni, Francesca; Bulgheroni, Elisabetta; Ferramosca, Stefania; Bencini, Andrea; Bianchi, Antonio; Ruiz, Lidia; Cabrera, Cecilia; Martinez-Picado, Javier; Supuran, Claudiu T.; Galli, Massimo. 2009. "New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses." Molecules 14, no. 5: 1927-1937.

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