کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1356834 981163 2008 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and heme-binding correlation with antimalarial activity of 3,6-bis-(ω-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and heme-binding correlation with antimalarial activity of 3,6-bis-(ω-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone
چکیده انگلیسی

In this study, the effect of fluorine upon the heme-binding ability of the xanthone nucleus was investigated for 3,6-bis-(ω-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone (F2C5). 2-Fluoro-1,3-dimethoxybenzene was prepared by a new, improved method and used to build up the xanthone nucleus. The interaction of F2C5 with heme was investigated by UV–vis, 1H NMR, and 19F NMR spectroscopy. For the first time, NMR studies for the heme–drug interactions are carried out at pH 5.0, physiological for the acidic food vacuole of the malaria parasite.

In this study, the synthesis and the heme-binding ability of a fluorine-containing xanthone are presented. 3,6-Bis-(ω-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone was designed to have enhanced affinity to heme and increased antimalarial potency.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 3, 1 February 2008, Pages 1174–1183
نویسندگان
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