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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
来源:
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.
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页码:522 / 526
页数:5
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