کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10594407 981826 2012 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers
چکیده انگلیسی
A series of macrocyclic compounds containing a cyclic constraint in the P2-P4 linker region have been discovered and shown to exhibit excellent HCV NS3/4a genotype 3a and genotype 1b R155 K, A156T, A156 V, and D168 V mutant activity while maintaining high rat liver exposure. The effect of the constraint is most dramatic against gt 1b A156 mutants where ∼20-fold improvements in potency are achieved by introduction of a variety of ring systems into the P2-P4 linker.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7207-7213
نویسندگان
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