کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10585258 981364 2012 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Febrifugine analogue compounds: Synthesis and antimalarial evaluation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Febrifugine analogue compounds: Synthesis and antimalarial evaluation
چکیده انگلیسی
Febrifugine is an alkaloid isolated from Dichroa febrifuga Lour as the active component against Plasmodium falciparum, but exhibits toxic side effects. In this study novel febrifugine analogues were designed and efficiently synthesized. New compounds underwent efficacy and toxicity evaluation. Some compounds are much less toxic than the natural product febrifugine and existing antimalarial drugs and are expected to possess wide therapeutic windows. In Aotus monkeys infected with the chloroquine resistant FVO strain of P. falciparum, one interesting compound possesses a 50% curative dose of 2 mg/kg/day and a 100% curative dose of 8 mg/kg/day. These compounds, as well as the underlying design rationale, may find usefulness in the discovery and development of new antimalarial drugs.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 2, 15 January 2012, Pages 927-932
نویسندگان
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