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Synthesis of potent and highly selective inhibitors of human tryptase
William A Slusarchyk1, Scott A Bolton, Karen S Hartl
1The Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. william.slusarchyk@bms.com
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
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 (IC(50)<1.7 nM) with high selectivity (>3000-fold) for tryptase versus related serine proteases including trypsin.