کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1394992 1501192 2010 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Original quinazoline derivatives displaying antiplasmodial properties
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Original quinazoline derivatives displaying antiplasmodial properties
چکیده انگلیسی

The multistep synthesis of new quinazoline-derived molecules and their in vitro antiplasmodial evaluation on the W2 chloroquino-resistant Plasmodium falciparum strain is described herein. These molecules have also been studied concerning their in vitro cytotoxicity toward two human cell lines (K652 and HepG2) in order to calculate their respective selectivity indexes (S.I.). Among the fourteen tested molecules, two exhibited both significant antiplasmodial activity (IC50 = 0.95 and 1.3 μM) and low toxicity (IC50 > 100 or 125 μM), compared with two reference drugs: chloroquine and doxycycline. The structure activity relationships establish that the molecular scaffold which exerts the best profile is the 6-nitro-2-(tosylmethyl)-N-(3-substituted-phenyl)-quinazolin-4-amine. The hit molecules were finally investigated regarding their potential action toward two other protozoa, Leishmania donovani and Toxoplasma gondii, showing that these molecules display a selective antiplasmodial activity.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 2, February 2010, Pages 616–622
نویسندگان
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