کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362136 981479 2010 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel nucleosides as potent influenza viral inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Novel nucleosides as potent influenza viral inhibitors
چکیده انگلیسی

Influenza virus infection constitutes a significant health problem in need of more effective therapies. We have recently identified ((2R,3S,4R,5R)-3-acetoxy-5-(4-benzamido-2-oxopyrimidin-1(2H)-yl)-4-fluoro-3,4-dimethyl-tetrahydrofuran-2-yl) methyl benzoate (18c) as a potent influenza virus inhibitor. We now here report the synthesis and evaluation of a series of C-3′ modified ribose nucleosides. These novel compounds were prepared, primarily by taking known ((2R,3R,4R)-3-benzoyloxy-4-fluoro-4-methyl-5-oxo-tetrahydrofuran-2-yl)methyl benzoate (1) and converting it in to C-3 keto sugar (7), reacting C-3 keto group with methyl magnesium bromide, followed by coupling these sugars with purine and pyrimidine bases. Anti influenza viral activity was determined by screening against both A and B viral strains.

Novel nucleosides were synthesized from di benzoyl fluoro lactone (1) and evaluated their anti-influenza viral activity. Compound (18c) showed the best antiviral activity among the compounds synthesized.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 17, 1 September 2010, Pages 6329–6339
نویسندگان
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