Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease

Bioorganic and Medicinal Chemistry Letters

Volumn 12, Issue 23, 2002, Pages 3359-3362

  Slater, Martin J ^a   Andrews, David M ^a   Baker, Graham ^a   Bethell, Susanne S ^a   Carey, Seb ^a   Chaignot, Helene ^a   Clarke, Berwyn ^a   Coomber, Barry ^a   Ellis, Malcolm ^a   Good, Andrew ^a   Gray, Norman ^a   Hardy, George ^a   Jones, Paul ^a   Mills, Gail ^a   Robinson, Ed ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

LACTAM DERIVATIVE; NITROGEN; PROTEINASE INHIBITOR; PYRROLINE DERIVATIVE; VIRUS PROTEIN; CARRIER PROTEIN; LACTAM; NS3 PROTEIN, HEPATITIS C VIRUS; NS4A COFACTOR PEPTIDE, HEPATITIS C VIRUS; PYRROLIDINE DERIVATIVE; SERINE PROTEINASE INHIBITOR;

ARTICLE; DRUG DESIGN; DRUG SYNTHESIS; HEPATITIS C VIRUS; IC 50; PROTEINASE INHIBITION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; VIRUS INHIBITION; AMINO ACID SEQUENCE; CHEMISTRY; DRUG ANTAGONISM; DRUG EFFECT; ENZYMOLOGY; HUMAN; METABOLISM; MICROBIOLOGICAL EXAMINATION; STEREOISOMERISM; SYNTHESIS;

HEPATITIS C VIRUS;

AMINO ACID SEQUENCE; CARRIER PROTEINS; DRUG DESIGN; HEPACIVIRUS; HUMANS; INHIBITORY CONCENTRATION 50; LACTAMS; MICROBIAL SENSITIVITY TESTS; PYRROLIDINES; SERINE PROTEINASE INHIBITORS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; VIRAL NONSTRUCTURAL PROTEINS; VIRAL PROTEINS;

EID: 0036888559     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(02)00789-8     Document Type: Article

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22. The detailed kinetics of enzyme inhibition and mechanism of action will be the subject of a separate publication.
23. m=5 μM.