Bioorganic & Medicinal Chemistry Letters 2000-10-16

Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.

K D Rice, A R Gangloff, E Y Kuo, J M Dener, V R Wang, R Lum, W S Newcomb, C Havel, D Putnam, L Cregar, M Wong, R L Warne

Index: Bioorg. Med. Chem. Lett. 10(20) , 2357-60, (2000)

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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.