SCH 503034, a Mechanism-Based Inhibitor of Hepatitis C Virus NS3 Protease, Suppresses Polyprotein Maturation and Enhances the Antiviral Activity of Alpha Interferon in Replicon Cells

Bruce A. Malcolm, R. Liu, Frederick Lahser, +19

Antimicrobial Agents and Chemotherapy

Viral ReplicationHepatitis C VirusImmunologyMolecular BiologyHcv Replication +15

Discovery of (1 <i>R</i> ,5 <i>S</i> )- <i>N</i> -[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2( <i>S</i> )-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2( <i>S</i> )-carboxamide (SCH 503034), a Selective, Potent, Orally Bioavailable Hepatitis C Virus NS3 Protease Inhibitor:  A Potential Therapeutic Agent for the Treatment of Hepatitis C Infection

Srikanth Venkatraman, Stéphane Bogen, Ashok Arasappan, +49

Journal of Medicinal Chemistry

Discovery of the HCV NS3/4A Protease Inhibitor (1<i>R</i>,5<i>S</i>)-<i>N</i>-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(<i>S</i>)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(<i>S</i>)-carboxamide (Sch 503034) II. Key Steps in Structure-Based Optimization

Andrew Prongay, Zhuyan Guo, Nanhua Yao, +28

Journal of Medicinal Chemistry

Protein AssemblyMolecular BiologyStructure-based OptimizationChemical BiologyPharmaceutical Chemistry +20

Enhancement of Hepatitis C Virus NS3 Proteinase Activity by Association with NS4A-Specific Synthetic Peptides: Identification of Sequence and Critical Residues of NS4A for the Cofactor Activity

Nancy Butkiewicz, Michelle Wendel, Rumin Zhang, +10

Virology

BiochemistryNatural SciencesNs4a-specific Synthetic PeptidesHepatitisMolecular Biology +6

Discovery of SCH446211 (SCH6):  A New Ketoamide Inhibitor of the HCV NS3 Serine Protease and HCV Subgenomic RNA Replication

Stéphane Bogen, Ashok Arasappan, Frank Bennett, +26

Journal of Medicinal Chemistry

Viral ReplicationImmunologyMolecular BiologyTranscriptional RegulationHcv Genome +14

Discovery and Structure−Activity Relationship of P₁−P₃ Ketoamide Derived Macrocyclic Inhibitors of Hepatitis C Virus NS3 Protease

Srikanth Venkatraman, Francisco Velázquez, Wanli Wu, +15

Journal of Medicinal Chemistry

Analogue 52Antiviral CompoundHepatologyBiochemistryViral Hepatitis +13

Preclinical Characterization of the Antiviral Activity of SCH 900518 (Narlaprevir), a Novel Mechanism-Based Inhibitor of Hepatitis C Virus NS3 Protease

Xiao Tong, Ashok Arasappan, Frank Bennett, +13

Antimicrobial Agents and Chemotherapy

ImmunologySch 900518Novel Mechanism-based InhibitorAntiviral DrugSmall Molecules +18

Potent 7-Hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic Acid-Based Macrocyclic Inhibitors of Hepatitis C Virus NS3 Protease

Kevin X. Chen, F. George Njoroge, John Pichardo, +5

Journal of Medicinal Chemistry

Medicinal ChemistryNs3 ProteaseBiochemistryMedicineNatural Sciences +11

Novel Potent Hepatitis C Virus NS3 Serine Protease Inhibitors Derived from Proline-Based Macrocycles

Kevin X. Chen, F. George Njoroge, Ashok Arasappan, +11

Journal of Medicinal Chemistry

Correlation between PAMPA permeability and cellular activities of hepatitis C virus protease inhibitors

Cheng Li, Latha G. Nair, Tongtong Liu, +10

Biochemical Pharmacology

Cellular ActivitiesViral HepatitisPampa PermeabilityMedicineImmunology +8