期刊
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
卷 31, 期 4, 页码 277-285出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/15257770.2012.658131
关键词
2 '-Deoxy-2 '-fluoro-2 '-C-methyluridine nucleotide; PSI-7851; PSI-7977; cyclopentyl carbocyclic uridine nucleoside; phosphoramidate prodrug; hepatitis C virus
The 2'-deoxy-2'-fluoro-2'-C-methyluridine nucleotide prodrug, PSI-7851 and its single diastereomer PSI-7977 have displayed potent antiviral activity against hepatitis C virus in clinical trials, and PSI-7977 is currently in Phase III studies. As part of our SAR study of the 2'-deoxy-2'-fluoro-2'-C-methyl class of nucleosides, we prepared the cyclopentyl carbocyclic uridine analog 11 and its phosphoramidate prodrug 15. Both 11 and 15 were shown not to inhibit HCV replication. This lack of activity might be attributed to the inability of the monophosphate to be converted to the corresponding diphosphate or triphosphate or the inactivity of triphosphate of 11 as an inhibitor of the polymerase.
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