کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375726 | 981943 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Twenty-four 4-hydroxypyrone derivatives were synthesized with a facile synthetic method to develop novel HIV protease inhibitors. Most of them were shown to display good antiviral activities in SIV-infected CEM cells. The introduction of α-naphthylmethyl group to C-6 of 5,6-dihydropyran-2-ones led to an effective antiviral compound that showed an EC50 value at 1.7 μM with a therapeutic index of 46.
Synthesis and biological evaluation of 24 4-hydroxypyrone derivatives are described. Compound 4C was the most potent inhibitor in this study, with an EC50 value at 1.7 μM and a therapeutic index of 46.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 13, 1 July 2005, Pages 3257–3262
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 13, 1 July 2005, Pages 3257–3262
نویسندگان
Chun-Lai Sun, Rui-Fang Pang, Hang Zhang, Ming Yang,