Document Detail


Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase.
MedLine Citation:
PMID:  19819138     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds were optimized to low nanomolar potencies in a biochemical RdRp assay. SAR trends clearly reveal a stringent preference for a cyclohexyl group as one of the hydrophobes, and improved activities for carboxylic acid derivatives.
Authors:
Janeta Popovici-Muller; Gerald W Shipps; Kristin E Rosner; Yongqi Deng; Tong Wang; Patrick J Curran; Meredith A Brown; M Arshad Siddiqui; Alan B Cooper; Jos?? Duca; Michael Cable; Viyyoor Girijavallabhan
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Publication Detail:
Type:  Journal Article     Date:  2009-09-25
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Nov 
Date Detail:
Created Date:  2009-10-26     Completed Date:  2010-01-27     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  6331-6     Citation Subset:  IM    
Affiliation:
Schering-Plough Research Institute Cambridge, 320 Bent Street, Cambridge, MA 02141, USA. janeta.popovici-muller@spcorp.com
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MeSH Terms
Descriptor/Qualifier:
DNA-Directed RNA Polymerases / antagonists & inhibitors*
Drug Evaluation, Preclinical
Enzyme Inhibitors / pharmacology*
Hepacivirus
Hepatitis C / enzymology*,  virology
Inhibitory Concentration 50
Molecular Weight
Pyrazoles / pharmacology*
Pyrimidines / pharmacology*
RNA Replicase / antagonists & inhibitors*
RNA, Viral / drug effects*
Small Molecule Libraries
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Pyrazoles; 0/Pyrimidines; 0/RNA, Viral; 0/Small Molecule Libraries; 0/pyrazolo(1,5-a)pyrimidine; EC 2.7.7.48/RNA Replicase; EC 2.7.7.6/DNA-Directed RNA Polymerases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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