Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl purine nucleosides as inhibitors of hepatitis C virus RNA replication.
A series of purine nucleosides containing the 2'-deoxy-2'-fluoro-2'-C-methylribofuranosyl moiety were synthesized and evaluated as potential inhibitors of the hepatitis C virus in vitro. Of the nucleosides that were synthesized, only those possessing a 2-amino group on the purine base reduced the levels of HCV RNA in a subgenomic replicon assay.
Clark
Jeremy L
JL
Pharmasset Inc., 1860 Montreal Road, Tucker, GA 30084, USA. j.clark@sri.org
Mason
J Christian
JC
Hollecker
Laurent
L
Stuyver
Lieven J
LJ
Tharnish
Phillip M
PM
McBrayer
Tamara R
TR
Otto
Michael J
MJ
Furman
Phillip A
PA
Schinazi
Raymond F
RF
Watanabe
Kyoichi A
KA
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D016174:Hepacivirus / Q000187:drug effects* / Q000235:genetics; D015394:Molecular Structure; D011684:Purine Nucleosides / Q000138:chemical synthesis / Q000494:pharmacology; D012367:RNA, Viral / Q000187:drug effects / Q000235:genetics; D012093:Replicon / Q000187:drug effects; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects*
D000998:Antiviral Agents; D011684:Purine Nucleosides; D012367:RNA, Viral