کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1374403 981918 2006 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of 4-substituted benzylamine derivatives as β-tryptase inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and evaluation of 4-substituted benzylamine derivatives as β-tryptase inhibitors
چکیده انگلیسی

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, c log P value less than 5, lack of amidino and guanidino groups, and independence of Zn2+ ion.

Synthesis and structure–activity relationships of β-tryptase inhibitors are described.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 11, 1 June 2006, Pages 2986–2990
نویسندگان
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