Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase

A series of tetrahydrobenzothiophenes have been prepared and identified as potent inhibitors of HCV NS5B polymerase. R = 6,6-Dimethyl, R′ = CONHSO 2Ar. A novel series of selective HCV NS5B RNA dependent RNA polymerase inhibitors has been disclosed. These compounds contain an appropriately substitute...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006, Vol.16 (1), p.100-103
Main Authors: LaPorte, M.G., Lessen, T.A., Leister, L., Cebzanov, D., Amparo, E., Faust, C., Ortlip, D., Bailey, T.R., Nitz, T.J., Chunduru, S.K., Young, D.C., Burns, C.J.
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Caco-2 Cells
Chemistry, Pharmaceutical - methods
Drug Design
Drug Evaluation, Preclinical
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
HCV polymerase inhibitors
Hepacivirus - enzymology
Humans
Medical sciences
Models, Chemical
Pharmacology. Drug treatments
Protein Structure, Tertiary
RNA-Dependent RNA Polymerase - antagonists & inhibitors
Structure-Activity Relationship
Sulfonamides - chemistry
Tetrahydrobenzothiophenes
Thiophenes - chemistry
Thiophenes - pharmacology
Viral Nonstructural Proteins - antagonists & inhibitors
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Summary:A series of tetrahydrobenzothiophenes have been prepared and identified as potent inhibitors of HCV NS5B polymerase. R = 6,6-Dimethyl, R′ = CONHSO 2Ar. A novel series of selective HCV NS5B RNA dependent RNA polymerase inhibitors has been disclosed. These compounds contain an appropriately substituted tetrahydrobenzothiophene scaffold. This communication will detail the SAR and activities of this series.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.09.047