کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372730 | 981879 | 2009 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of tricyclic 5,6-dihydro-1H-pyridin-2-ones as novel, potent, and orally bioavailable inhibitors of HCV NS5B polymerase
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of non-nucleoside small molecules containing a tricyclic dihydropyridinone structural motif was identified as potent HCV NS5B polymerase inhibitors. Driven by structure-based design and building on our previous efforts in related series of molecules, we undertook extensive SAR studies, in which we identified a number of metabolically stable and very potent compounds in genotype 1a and 1b replicon assays. This work culminated in the discovery of several inhibitors, which combined potent in vitro antiviral activity against both 1a and 1b genotypes, metabolic stability, good oral bioavailability, and high C12 (PO)/EC50 ratios.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 22, 15 November 2009, Pages 6404–6412
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 22, 15 November 2009, Pages 6404–6412
نویسندگان
Frank Ruebsam, Douglas E. Murphy, Chinh V. Tran, Lian-Sheng Li, Jingjing Zhao, Peter S. Dragovich, Helen M. McGuire, Alan X. Xiang, Zhongxiang Sun, Benjamin K. Ayida, Julie K. Blazel, Sun Hee Kim, Yuefen Zhou, Qing Han, Charles R. Kissinger,