• Title of article

    Erratum to “Synthesis of potent and selective 2-azepanone inhibitors of human tryptase” Biorg. Med. Chem. Lett. 14 (2004) 309

  • Author/Authors

    Guohua Zhao، نويسنده , , ScottA Bolton، نويسنده , , Chet Kwon، نويسنده , , KarenS Hartl، نويسنده , , StevenM Seiler، نويسنده , , WilliamA Slusarchyk، نويسنده , , JamesC Sutton، نويسنده , , GregoryS Bisacchi، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2004
  • Pages
    1
  • From page
    1057
  • To page
    1057
  • Abstract
    The serine protease tryptase has been associated with a broad range of allergic and inflammatory diseases and, in particular, has been implicated as a critical mediator of asthma. The inhibition of tryptase therefore has the potential to be a valuable therapy for asthma. The synthesis, employing solution phase parallel methods, and SAR of a series of novel 2-azepanone tryptase inhibitors are presented. A member of this series, 8t, was identified as a potent inhibitor of human tryptase (IC50=38 nM) with selectivity ≥330-fold versus related serine proteases (trypsin, plasmin, uPA, tPA, APC, alpha-thrombin, and FXa).
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2004
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    794131