Document Report Card

Basic Information

ID: ALA1132783

Journal: Bioorg Med Chem Lett

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

Authors: Rice KD, Gangloff AR, Kuo EY, Dener JM, Wang VR, Lum R, Newcomb WS, Havel C, Putnam D, Cregar L, Wong M, Warne RL.

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.

CiteXplore: 11055355

DOI: 10.1016/s0960-894x(00)00484-4