کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1355879 981070 2012 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Investigating the activity of quinine analogues versus chloroquine resistant Plasmodium falciparum
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Investigating the activity of quinine analogues versus chloroquine resistant Plasmodium falciparum
چکیده انگلیسی

Plasmodium falciparum, the deadliest malarial parasite species, has developed resistance against nearly all man-made antimalarial drugs within the past century. However, quinine (QN), the first antimalarial drug, remains efficacious worldwide. Some chloroquine resistant (CQR) P. falciparum strains or isolates show mild cross resistance to QN, but many do not. Further optimization of QN may provide a well-tolerated therapy with improved activity versus CQR malaria. Thus, using the Heck reaction, we have pursued a structure–activity relationship study, including vinyl group modifications of QN. Certain derivatives show good antiplasmodial activity in QN-resistant and QN-sensitive strains, with lower IC50 values relative to QN.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 10, 15 May 2012, Pages 3292–3297
نویسندگان
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