کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1360241 981432 2009 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines
چکیده انگلیسی

To identify a new safe antiplasmodial molecular scaffold, an original series of 2-trichloromethylquinazolines, functionalized in position 4 by an alkyl- or arylamino substituent, was synthesized from 4-chloro-2-trichloromethylquinazoline 1, via a cheap, fast and efficient solvent-free operating procedure. Among the 40 molecules prepared, several exhibit a good profile with both a significant antiplasmodial activity on the W2 Plasmodium falciparum strain (IC50 values: 0.4–2.2 μM) and a promising toxicological behavior regarding human cells (HepG2/W2 selectivity indexes: 40–83), compared to the antimalarial drug compounds chloroquine and doxycycline. The in vitro antitoxoplasmic and antileishmanial evaluations were conducted in parallel on the most active molecules, showing that these ones specifically display antiplasmodial properties.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 13, 1 July 2009, Pages 4313–4322
نویسندگان
, , , , , , , , , , ,