Synthesis and evaluation of 4-substituted benzylamine derivatives as β-tryptase inhibitors

…, T Egusa, M Ohkouchi, I Shiromizu, T Matsusue…

Index: Miyazaki, Yutaka; Kato, Yutaka; Manabe, Tadashi; Shimada, Hiroyasu; Mizuno, Masashi; Egusa, Takayuki; Ohkouchi, Munetaka; Shiromizu, Ikuya; Matsusue, Tomokazu; Yamamoto, Ichiro Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 11 p. 2986 - 2990

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Citation Number: 5

Abstract

Since β-tryptase is considered a critical mediator of asthma, potent tryptase inhibitors may be useful as new agents for the treatment of asthma. We investigated 4-substituted benzylamine derivatives and obtained M58539 (15h) as a potent inhibitor of β-tryptase (IC50= 5.0 nM) with high selectivity against other serine proteases, low molecular weight, clogP value less than 5, lack of amidino and guanidino groups, and independence of ...