Document Report Card
Basic Information
ID: ALA1132784
Journal: Bioorg Med Chem Lett
Title: Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.
Authors: Rice KD, Wang VR, Gangloff AR, Kuo EY, Dener JM, Newcomb WS, Young WB, Putnam D, Cregar L, Wong M, Simpson PJ.
Abstract: Detailed structure activity relationships (SARs) for a series of dibasic human tryptase inhibitors are presented. The structural requirements for potent inhibitory activity are remarkably broad with a range of core template modifications being well tolerated. Optimized inhibitors demonstrate potent anti-asthmatic activity in a sheep model of allergic asthma. APC-2059, a dibasic tryptase inhibitor with subnanomolar activity, has been advanced to phase II clinical trials for the treatment of both psoriasis and ulcerative colitis.
CiteXplore: 11055356