کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10585131 981362 2012 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and antimalarial activity of new haemanthamine-type derivatives
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and antimalarial activity of new haemanthamine-type derivatives
چکیده انگلیسی
Thirty one derivatives were prepared from the natural alkaloids haemanthamine (1), haemanthidine (2) and 11-hydroxyvittatine (3). They were evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum and some structure-activity relationships were outlined. For haemanthamine derivatives having a methoxy group at C-3, the presence of a free hydroxyl group at C-11 is important for the activity. The double bond at C-1-C-2 plays also an important role to achieve good inhibitory activity. Compound 35 with two nicotinate groups at C-3 and at C-11 was the most active compound with a IC50 = 0.8 ± 0.06 μM.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 18, 15 September 2012, Pages 5464-5472
نویسندگان
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