کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369787 | 981789 | 2012 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of new potent and selective HCV NS5A inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
NS5A inhibitors are a new class of direct-acting antiviral agents which display very potent anti-HCV activity in vitro and in humans. Rationally designed modifications to the central biphenyl linkage of a known NS5A series led to selection of several compounds that were synthesized and evaluated in a HCV genotype 1b replicon. The straight triphenyl linked compound 11a showed similar anti-HCV activity to the clinical compound BMS-790052 and a superior cytotoxicity profile in three different cell lines, with an EC50 value of 26 pM and a therapeutic index of over four million in an HCV replicon assay. This triphenyl analog warrants further preclinical evaluation as an anti-HCV agent.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 10, 15 May 2012, Pages 3488–3491
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 10, 15 May 2012, Pages 3488–3491
نویسندگان
Junxing Shi, Longhu Zhou, Franck Amblard, Drew R. Bobeck, Hongwang Zhang, Peng Liu, Lavanya Bondada, Tamara R. McBrayer, Phillip M. Tharnish, Tony Whitaker, Steven J. Coats, Raymond F. Schinazi,