کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373426 1500544 2010 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease
چکیده انگلیسی

HCV NS3/4A serine protease is essential for the replication of the HCV virus and has been a clinically validated target. A series of HCV NS3/4A protease inhibitors containing a novel acylsulfamoyl benzoxaborole moiety at the P1′ region was synthesized and evaluated. The resulting P1–P3 and P2–P4 macrocyclic inhibitors exhibited sub-nanomolar potency in the enzymatic assay and low nanomolar activity in the cell-based replicon assay. The in vivo PK evaluations of selected compounds are also described.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 24, 15 December 2010, Pages 7493–7497
نویسندگان
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