| Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase. | |
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MedLine Citation:
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PMID: 18487044 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Pyrrolo[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Structure-based design led to the discovery of compound 3 k, which displayed potent inhibitory activities in biochemical and replicon assays (IC(50) (1b)<10nM; EC(50) (1b)=12 nM) as well as good stability towards human liver microsomes (HLM t(1/2)>60 min). |
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Authors:
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Frank Ruebsam; Stephen E Webber; Martin T Tran; Chinh V Tran; Douglas E Murphy; Jingjing Zhao; Peter S Dragovich; Sun Hee Kim; Lian-Sheng Li; Yuefen Zhou; Qing Han; Charles R Kissinger; Richard E Showalter; Matthew Lardy; Amit M Shah; Mei Tsan; Rupal Patel; Laurie A Lebrun; Ruhi Kamran; Maria V Sergeeva; Darian M Bartkowski; Thomas G Nolan; Daniel A Norris; Leo Kirkovsky |
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Publication Detail:
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Type: Journal Article Date: 2008-05-01 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 18 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2008 Jun |
Date Detail:
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Created Date: 2008-06-10 Completed Date: 2008-08-25 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3616-21 Citation Subset: IM |
Affiliation:
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Anadys Pharmaceuticals, Inc., 3115 Merryfield Row, San Diego, CA 92121, USA. fruebsam@anadyspharma.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antiviral Agents / chemical synthesis, chemistry, pharmacology* Binding Sites / drug effects Cell Line Crystallography, X-Ray Humans Hydrogen Bonding Microbial Sensitivity Tests Models, Molecular Molecular Structure Pyridazines / chemical synthesis, chemistry, pharmacology* Pyrroles / chemical synthesis, chemistry, pharmacology* Structure-Activity Relationship Viral Nonstructural Proteins / antagonists & inhibitors*, chemistry |
| Chemical | |
Reg. No./Substance:
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0/Antiviral Agents; 0/NS-5 protein, hepatitis C virus; 0/Pyridazines; 0/Pyrroles; 0/Viral Nonstructural Proteins |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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