Document Detail


Potent aza-peptide derived inhibitors of HCV NS3 protease.
MedLine Citation:
PMID:  19596195     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Chronic hepatitis C infection is the primary cause for cirrhosis of the liver and hepatocellular carcinoma leading to liver failure and transplantation. The etiological agent hepatitis C virus produces a single positive strand RNA that is processed further with the help of NS3 serine protease to produce mature virus. Inhibition of this protease can potentially be used to develop drugs for HCV infections. Boceprevir is a ketoamide derived novel inhibitor of HCV NS3 protease that has been progressed to clinical trials and proven to be efficacious in humans. Herein, we report our efforts in identifying an aza-peptide derivative as a potential second generation compound, that lacks electrophilic ketoamide group and are potent in enzyme and replicon assay.
Authors:
Srikanth Venkatraman; Wanli Wu; Neng-Yang Shih; F George Njoroge
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Publication Detail:
Type:  Journal Article     Date:  2009-06-17
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Aug 
Date Detail:
Created Date:  2009-07-29     Completed Date:  2009-10-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  4760-3     Citation Subset:  IM    
Affiliation:
Schering Plough Research Institute, K15-MS 3545, Kenilworth, NJ 07033, United States. Srikanth.Venkatraman@spcorp.com
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MeSH Terms
Descriptor/Qualifier:
Antiviral Agents / chemical synthesis,  chemistry*,  pharmacology
Aza Compounds / chemical synthesis,  chemistry*,  pharmacology
Hepacivirus / enzymology*
Hepatitis C / drug therapy
Humans
Peptides / chemical synthesis,  chemistry*,  pharmacology
Serine Proteinase Inhibitors / chemical synthesis,  chemistry*,  pharmacology
Viral Nonstructural Proteins / antagonists & inhibitors*,  metabolism
Chemical
Reg. No./Substance:
0/Antiviral Agents; 0/Aza Compounds; 0/NS3 protein, hepatitis C virus; 0/Peptides; 0/Serine Proteinase Inhibitors; 0/Viral Nonstructural Proteins

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