کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595038 981854 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vitro and in vivo antimalarial evaluation of semi-synthetic derivatives of gomphostenin
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
In vitro and in vivo antimalarial evaluation of semi-synthetic derivatives of gomphostenin
چکیده انگلیسی
A novel series of semi-synthetic gomphostenin derivatives (1 to 9) were prepared utilizing C-14 hydroxyl group for the first time and studied for their antimalarial properties. In vitro antiplasmodial activity was evaluated against both the chloroquine-sensitive and resistant strains of Plasmodium falciparum. Most of the compounds exhibited superior or comparable antiplasmodial activity compared to parent compound i.e. gomphostenin (GN). Based upon in vitro antiplasmodial activity, compounds with IC50 values less than 10 μM were selected for in vivo antiplasmodial evaluation against Plasmodium berghei infection in mice model. GN derivatives 3 and 5 were found to have curative activity with moderate chemosupression of 65% and 69% respectively at the dose level of 150 mg/kg/day.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 14, 15 July 2010, Pages 4233-4236
نویسندگان
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