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Tricyclic 2′-C-Modified Nucleosides as Potential Anti-HCV Therapeutics
被引:19
作者:
Wauchope, Orrette R.
[2
]
Tomney, Matthew J.
[2
]
Pepper, Joseph L.
[2
]
Korba, Brent E.
[1
]
Seley-Radtke, Katherine L.
[1
]
机构:
[1] Georgetown Univ, Med Ctr, Dept Microbiol & Immunol, Washington, DC 20057 USA
[2] Univ Maryland, Dept Chem & Biochem, Baltimore, MD 21250 USA
关键词:
C VIRUS-REPLICATION;
INHIBITORS;
DESIGN;
D O I:
10.1021/ol101482h
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
Promising biological activity in a number of therapeutic areas has been reported for both tricyclic nucleosides and 2'-modified nucleosides. In particular, disubstitution at the C-2' position of nucleosides has resulted in significant activity against the hepatitis C virus (HCV). Combining this with the observation that tricyclic nucleosides developed in our laboratory have been shown to inhibit the RNA-dependent RNA polymerase NS5B led to the design of a series of 2'-modified tricyclic nucleosides. Details of the synthesis, structural characterization, and preliminary biological results are reported.
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页码:4466 / 4469
页数:4