| Literature DB >> 12372541 |
William A Slusarchyk1, Scott A Bolton, Karen S Hartl, Ming-Hsing Huang, Glenn Jacobs, Wei Meng, Martin L Ogletree, Zulan Pi, William A Schumacher, Steven M Seiler, James C Sutton, Uwe Treuner, Robert Zahler, Guohua Zhao, Gregory S Bisacchi.
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.Entities:
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Year: 2002 PMID： 12372541 DOI： 10.1016/s0960-894x(02)00689-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823