Title of article
Synthesis of potent and highly selective inhibitors of human tryptase
Author/Authors
William A. Slusarchyk، نويسنده , , Scott A. Bolton، نويسنده , , Karen S. Hartl، نويسنده , , Ming-Hsing Huang، نويسنده , , Glenn Jacobs، نويسنده , , Wei Meng، نويسنده , , Martin L. Ogletree، نويسنده , , Zulan Pi، نويسنده , , William A. Schumacher، نويسنده , , Steven M. Seiler، نويسنده , , James C. Sutton، نويسنده , , Uwe Treuner، نويسنده , , Robert Zahler، نويسنده , , Guohua Zhao، نويسنده , , Gregory S. Bisacchi، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
3235
To page
3238
Abstract
The serine protease tryptase has been implicated in allergic and inflammatory diseases and associated with asthma. The synthesis and SAR of a series of N1-activated-4-carboxy azetidinones are described, resulting in identification of BMS-363131 (2) as a potent inhibitor of human tryptase (IC50<1.7 nM) with high selectivity (>3000-fold) for tryptase versus related serine proteases including trypsin.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792640
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