Bioorganic and Medicinal Chemistry Letters p. 2361 - 2366 (2000)
Update date:2022-09-26
Topics:
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.
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.
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