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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2004-3-18
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pubmed:abstractText |
From the discovery of competitive hexapeptide inhibitors, potent and selective HCV NS3 protease macrocyclic inhibitors have been identified. Structure-activity relationship studies were performed focusing on optimizing the N-terminal carbamate and the aromatic substituent on the (4R)-hydroxyproline moiety. Inhibitors meeting the potency criteria in the cell-based assay and with improved oral bioavailability in rats were identified. BILN 2061 was selected as the best compound, the first NS3 protease inhibitor reported with antiviral activity in man.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BaileyMurray DMD,
pubmed-author:BolgerGordonG,
pubmed-author:BrochuChristianC,
pubmed-author:FaucherAnne-MarieAM,
pubmed-author:FerlandJean MarieJM,
pubmed-author:GarneauMichelM,
pubmed-author:GhiroEliseE,
pubmed-author:GorysVidaV,
pubmed-author:Grand-MaîtreChantalC,
pubmed-author:HalmosTedT,
pubmed-author:LamarreDanielD,
pubmed-author:Lapeyre-PaquetteNicoleN,
pubmed-author:LiardFrancineF,
pubmed-author:Llinàs-BrunetMontseM,
pubmed-author:PoirierMartinM,
pubmed-author:RhéaumeManonM,
pubmed-author:TsantrizosYoula SYS
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1605-8
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pubmed:meshHeading |
pubmed-meshheading:15027850-Administration, Oral,
pubmed-meshheading:15027850-Animals,
pubmed-meshheading:15027850-Antiviral Agents,
pubmed-meshheading:15027850-Biological Availability,
pubmed-meshheading:15027850-Carbamates,
pubmed-meshheading:15027850-Hepacivirus,
pubmed-meshheading:15027850-Heterocyclic Compounds,
pubmed-meshheading:15027850-Injections, Intravenous,
pubmed-meshheading:15027850-Proline,
pubmed-meshheading:15027850-Protease Inhibitors,
pubmed-meshheading:15027850-Rats,
pubmed-meshheading:15027850-Structure-Activity Relationship,
pubmed-meshheading:15027850-Viral Nonstructural Proteins
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pubmed:year |
2004
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pubmed:articleTitle |
Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061.
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pubmed:affiliation |
Department of Chemistry, Boehringer Ingelheim (Canada) Ltd., 2100 Cunard Street, Laval, Québec H7S 2G5, Canada. mllinas@lav.boehringer-ingelheim.com
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pubmed:publicationType |
Journal Article
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