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  • Title: Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
    Author: Hopkins C, Neuenschwander K, Scotese A, Jackson S, Nieduzak T, Pauls H, Liang G, Sides K, Cramer D, Cairns J, Maignan S, Mathieu M.
    Journal: Bioorg Med Chem Lett; 2004 Oct 04; 14(19):4819-23. PubMed ID: 15341931.
    Abstract:
    In this manuscript, the synthesis and SAR evaluation of a novel pyrazinone class of tryptase inhibitors is described. Chemical optimization of the P1 and P4 groups led to the identification of 7p (K(i)=93 nM) as a potent inhibitor of mast cell tryptase.
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