کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373589 | 981903 | 2007 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and antiviral properties of 4′-substituted ribonucleosides as inhibitors of hepatitis C virus replication: The discovery of R1479
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 4′-substituted ribonucleoside derivatives has been prepared and evaluated for inhibition of hepatitis C virus (HCV) RNA replication in cell culture. The most potent and non-cytotoxic derivative was compound 28 (4′-azidocytidine, R1479) with an IC50 of 1.28 μM in the HCV replicon system. The triphosphate of compound 28 was prepared and shown to be an inhibitor of RNA synthesis mediated by NS5B (IC50 = 320 nM), the RNA polymerase encoded by HCV. Data on related analogues have been used to generate some preliminary requirements for activity within this series of nucleosides.
The synthesis of 4′-substituted nucleosides as potential antiviral agents is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2570–2576
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2570–2576
نویسندگان
David B. Smith, Joseph A. Martin, Klaus Klumpp, Stewart J. Baker, Peter A. Blomgren, Rene Devos, Caroline Granycome, Julie Hang, Christopher J. Hobbs, Wen-Rong Jiang, Carl Laxton, Sophie Le Pogam, Vincent Leveque, Han Ma, Graham Maile, John H. Merrett,