178972-27-5Relevant academic research and scientific papers
Dibasic inhibitors of human mast cell tryptase. Part 2: Structure-activity relationships and requirements for potent activity
Rice, Kenneth D.,Wang, Vivian R.,Gangloff, Anthony R.,Kuo, Elaine Y.-L.,Dener, Jeffrey M.,Newcomb, William S.,Young, Wendy B.,Putnam, Daun,Cregar, Lynne,Wong, Martin,Simpson, Paul J.
, p. 2361 - 2366 (2000)
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. (C) 2000 Published by Elsevier Science Ltd.
