کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364168 981530 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Inhibitors of hepatitis C virus NS3/4A: α-Ketoamide based macrocyclic inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Inhibitors of hepatitis C virus NS3/4A: α-Ketoamide based macrocyclic inhibitors
چکیده انگلیسی

A novel series of hepatitis C virus (HCV) NS3/4A protease inhibitors bearing a P2-P4 macrocycle and a P1-P1′ α-ketoamide serine trap is reported. The NS3 protease, which is essential for viral replication, is considered one of the most attractive targets for developing novel anti-HCV therapies. The optimization of both the macrocycle and the warhead portions led to the discovery of compounds 8b and 8g with a good activity both in the enzyme as well as in the cell based (replicon) assays with favorable PK profile in a preclinical species.

Design, synthesis and biological evaluation of a new series of hepatitis C virus (HCV) NS3/4A protease inhibitors bearing a P2-P4 macrocycle and a P1-P1′ α-ketoamide warhead is described.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 8, 15 April 2009, Pages 2295–2298
نویسندگان
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