Document Detail


Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.
MedLine Citation:
PMID:  18487044     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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).
Authors:
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:
Type:  Journal Article     Date:  2008-05-01
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  18     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2008 Jun 
Date Detail:
Created Date:  2008-06-10     Completed Date:  2008-08-25     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3616-21     Citation Subset:  IM    
Affiliation:
Anadys Pharmaceuticals, Inc., 3115 Merryfield Row, San Diego, CA 92121, USA. fruebsam@anadyspharma.com
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MeSH Terms
Descriptor/Qualifier:
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:
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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