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Synthesis of 3′-halo-5′-norcarbocyclic nucleoside phosphonates as potent anti-HIV agents
Journal article   Peer reviewed

Synthesis of 3′-halo-5′-norcarbocyclic nucleoside phosphonates as potent anti-HIV agents

Nadège Hamon, Malika Kaci, Jean-Pierre Uttaro, Christian Périgaud and Christophe Mathé
European Journal of Medicinal Chemistry, Vol.150, pp.642-654
04/2018
PMID: 29558735

Abstract

Antiviral Carbocycle HIV Nucleoside analogues Phosphonates Anti-HIV Agents Dose-Response Relationship, Drug HIV-1 Humans Leukocytes, Mononuclear Molecular Structure Nucleosides Organophosphonates Structure-Activity Relationship Virus Replication
The synthesis and the antiviral evaluation of 3'-halo (iodo and fluoro) 5'-norcarbocyclic nucleoside phosphonates is described. No antiviral activity was observed against Zika virus, Dengue virus 2, HSV-1, HSV-2 and Chikungunya virus. In contrast, some of the synthesized compounds are potent inhibitors of the replication of HIV-1, comparatively to (R)-PMPA, with no concomitant cytotoxicity.
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