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. 2018 Apr 25:150:642-654.
doi: 10.1016/j.ejmech.2018.03.038. Epub 2018 Mar 14.

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

Nadège Hamon  1 , Malika Kaci  1 , Jean-Pierre Uttaro  1 , Christian Périgaud  1 , Christophe Mathé  2
Affiliations

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

Nadège Hamon et al. Eur J Med Chem. .

Abstract

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.

Keywords: Antiviral; Carbocycle; HIV; Nucleoside analogues; Phosphonates.

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