کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371880 981857 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)
چکیده انگلیسی

In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provided compounds in which the amidine, binding in the S1 pocket, was replaced with a primary amine. Further modifications led to the identification of potent, selective, and orally bioavailable uPA inhibitors.

The discovery, synthesis, and early SAR work on a benzyl amine containing series of uPA inhibitors is reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 19, 1 October 2009, Pages 5712–5715
نویسندگان
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