Synthesis of 9-(2-β- C-methyl-β- d-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication

[Display omitted] A series of 9-(2′-β- C-methyl-β- d-ribofuranosyl)-6-substituted purine derivatives were synthesized as potential inhibitors of HCV RNA replication. Their inhibitory activities in a cell based HCV replicon assay were reported. A prodrug approach was used to further improve the poten...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (3), p.709-713
Main Authors: Ding, Yili, Girardet, Jean-Luc, Hong, Zhi, Lai, Vicky C.H., An, Haoyun, Koh, Yung-hyo, Shaw, Stephanie Z., Zhong, Weidong
Format: Article
Language:English
Subjects:
2- C-Methyl nucleoside
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - chemical synthesis
Biological and medical sciences
Cell Line
HCV
Hepacivirus - genetics
Humans
Inhibitors
Medical sciences
Pharmacology. Drug treatments
Prodrugs - chemical synthesis
Prodrugs - pharmacology
Purine Nucleosides - chemical synthesis
Purine Nucleosides - pharmacology
Replicon - drug effects
RNA, Viral - drug effects
RNA, Viral - genetics
Structure-Activity Relationship
Virus Replication - drug effects
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Summary:[Display omitted] A series of 9-(2′-β- C-methyl-β- d-ribofuranosyl)-6-substituted purine derivatives were synthesized as potential inhibitors of HCV RNA replication. Their inhibitory activities in a cell based HCV replicon assay were reported. A prodrug approach was used to further improve the potency of these compounds by increasing the intracellular levels of 5′-monophosphate metabolites. These nucleotide prodrugs showed much improved inhibitory activities of HCV RNA replication.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.11.020