Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034

Substitutions on the P 1 cyclobutyl side chain of SCH 503034 were studied by introduction of hydroxyl and fluoro substituents. Additionally, effects of fluoro substitution on other P1 moieties were evaluated.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-07, Vol.18 (14), p.4219-4223
Main Authors: Bogen, S., Arasappan, A., Pan, W., Ruan, S., Padilla, A., Saksena, A.K., Girijavallabhan, V., Njoroge, F.G.
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Area Under Curve
Biological and medical sciences
Chemistry, Pharmaceutical - methods
Drug Design
Fluorinated P1
Fluorine - chemistry
HCV protease inhibitor
Hepatitis C - drug therapy
Hepatitis C virus
Humans
Inhibitory Concentration 50
Kinetics
Medical sciences
Models, Chemical
Molecular Conformation
Pharmacology. Drug treatments
PK properties
Proline - analogs & derivatives
Proline - chemical synthesis
Proline - pharmacology
SCH 503034
Serine Proteinase Inhibitors - chemical synthesis
Serine Proteinase Inhibitors - pharmacology
Stereoisomerism
Structure-Activity Relationship
Viral Nonstructural Proteins - antagonists & inhibitors
Viral Nonstructural Proteins - chemistry
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Description
Summary:Substitutions on the P 1 cyclobutyl side chain of SCH 503034 were studied by introduction of hydroxyl and fluoro substituents. Additionally, effects of fluoro substitution on other P1 moieties were evaluated.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.05.060