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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors
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
نویسندگان
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