Synthesis and Antiviral Evaluation of 3′-Fluoro-4′-modified-5′-norcarbocyclic Nucleoside Phosphonates

被引:3
作者
Geant, Pierre-Yves [1 ]
Kaci, Malika [1 ]
Uttaro, Jean-Pierre [1 ]
Perigaud, Christian [1 ]
Mathe, Christophe [1 ]
机构
[1] Univ Montpellier, CNRS, UMR 5247, ENSCM,IBMM, Cc 1705,Site Triolet,Pl Eugene Bataillon, F-34095 Montpellier 5, France
关键词
3 '-fluoro-5 '-norcarbocyclic nucleosides; anti-HIV; antiviral agents; phosphonates; HIV; ANALOGS;
D O I
10.1002/cmdc.201800804
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and anti-HIV evaluation of hitherto unknown 3 '-fluoro-5 '-norcarbocyclic nucleoside phosphonates bearing adenine with modifications at the 4 ' position (ethynyl, vinyl, ethyl, hydroxymethyl) is described. One of the synthesized compounds was found to be an inhibitor of HIV-1 replication, but with moderate efficiency relative to (R)-9-(2-phosphonylmethoxypropyl)adenine ((R)-PMPA, tenofovir), with no concomitant cytotoxicity.
引用
收藏
页码:522 / 526
页数:5
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