Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase

A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase. A number of these compounds exhibited potent activity in enzymatic assay. The synthesis and structure-activity relationship are also describe...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5363-5367
Main Authors: YONGQI DENG, SHIPPS, Gerald W, TONG WANG, POPOVICI-MULLER, Janeta, ROSNER, Kristin E, ARSHAD SIDDIQUI, M, DUCA, Jose, COOPER, Alan B, CABLE, Michael
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Biological and medical sciences
Hepacivirus - enzymology
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Protein Binding
Pyrazoles - chemistry
Pyrazoles - pharmacology
Pyrimidines - chemistry
Pyrimidines - pharmacology
RNA-Dependent RNA Polymerase - antagonists & inhibitors
RNA-Dependent RNA Polymerase - metabolism
Structure-Activity Relationship
Viral Nonstructural Proteins - antagonists & inhibitors
Viral Nonstructural Proteins - metabolism
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Summary:A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase. A number of these compounds exhibited potent activity in enzymatic assay. The synthesis and structure-activity relationship are also described.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.07.124