کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373183 981891 2011 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors
چکیده انگلیسی

A novel 1,3,5-trisubstituted benzamide thrombin inhibitor template was designed via hybridization of a known aminopyridinoneacetamide and a known 1,3,5-trisubstituted phenyl ether. Optimization of this lead afforded a novel potent series of biaryl 1,3,5-trisubstituted benzenes with excellent functional anticoagulant potency.

Structure based design techniques were used to exploit the putative similarity in binding mode of an aminopyridinone thrombin inhibitor 2 and a trisubstituted benzene inhibitor 3 to generate a new lead inhibitor 4. Further optimization led to the identification of a novel series of potent thrombin inhibitor 22 with improved physical, chemical stability and in vitro functional potency.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1536–1540
نویسندگان
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