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  • Title: Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.
    Author: Miyazaki Y, Kato Y, Manabe T, Shimada H, Mizuno M, Egusa T, Ohkouchi M, Shiromizu I, Matsusue T, Yamamoto I.
    Journal: Bioorg Med Chem Lett; 2006 Jun 01; 16(11):2986-90. PubMed ID: 16540315.
    Abstract:
    Since beta-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 beta-tryptase (IC50 = 5.0 nM) with high selectivity against other serine proteases, low molecular weight, clog P value less than 5, lack of amidino and guanidino groups, and independence of Zn2+ ion.
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