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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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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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cited_by	cdi_FETCH-LOGICAL-c332t-8d37a56ecf86b233255e098b21543d9d7f69ad9022f992d77c9613f1b2faec433
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container_title	Bioorganic & medicinal chemistry letters
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creator	YONGQI DENG SHIPPS, Gerald W TONG WANG POPOVICI-MULLER, Janeta ROSNER, Kristin E ARSHAD SIDDIQUI, M DUCA, Jose COOPER, Alan B CABLE, Michael
description	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.
doi_str_mv	10.1016/j.bmcl.2009.07.124
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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
title	Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase
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