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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters