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  • Title: Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.
    Author: Rice KD, Gangloff AR, Kuo EY, Dener JM, Wang VR, Lum R, Newcomb WS, Havel C, Putnam D, Cregar L, Wong M, Warne RL.
    Journal: Bioorg Med Chem Lett; 2000 Oct 16; 10(20):2357-60. PubMed ID: 11055355.
    Abstract:
    The synthesis and optimization of a novel class of reversible and active-site directed dibasic inhibitors of human mast cell tryptase are described. The compounds were shown to be both remarkably potent and selective for tryptase with Ki values for optimized inhibitors in the picomolar range.
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