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steps towards sch503034 boceprevir. a ns3

The HCV Life Cycle. . NS3 Protease. NS3. . . . . . . . . . . . Positive strand RNA virusGenome encodes a single polyproteinNS3 cleaves 4 downstream sitesSerine protease Active site shallow and hydrophobic. HCV Genome Organization. Structural Proteins. NS3 protease inhibitors. hydrolysis. Electrophilic inhibition.

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steps towards sch503034 boceprevir. a ns3

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    1. Steps Towards Sch503034 (Boceprevir). A NS3/4A Protease Inhibitor as a Potential Treatment for Hepatitis C

    3. Positive strand RNA virus Genome encodes a single polyprotein NS3 cleaves 4 downstream sites Serine protease Active site shallow and hydrophobic

    4. NS3 protease inhibitors

    5. Spectrophotometric Progress Curve Analysis of Ketoamides

    6. Substrate- Based HCV Inhibitors

    7. P’ Truncated Compounds

    8. X-Ray Structure of Cpd 2

    11. Truncated Analogs

    12. Optimization of P1 in Primary Amide Series

    13. Modications of Proline at P2

    14. Synergistic Effects In the P1 Cyclopropyl Series

    15. Synergistic Effects In the P1 Cyclobutyl Series

    17. Synthesis of Sch 503034 - P1 Segment

    18. Synthesis of Sch 503034 (Cont’d)

    19. Profile of Sch 503034 - The Clinical Compound

    20. Summary of Truncations

    21. SCH 503034 Monotherapy 14 DaysHCV-1 IFN NRs, Mean Log10 Decrease HCV-RNA

    22. SCH 503034 ± PEG-Intron 1.5 mg/kg QW in HCV-1, IFN Non-Responders

    23. Summary

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