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  • Title: Synthesis of potent and highly selective inhibitors of human tryptase.
    Author: Slusarchyk WA, Bolton SA, Hartl KS, Huang MH, Jacobs G, Meng W, Ogletree ML, Pi Z, Schumacher WA, Seiler SM, Sutton JC, Treuner U, Zahler R, Zhao G, Bisacchi GS.
    Journal: Bioorg Med Chem Lett; 2002 Nov 04; 12(21):3235-8. PubMed ID: 12372541.
    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.
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