کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595942 981883 2013 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Borrelidin analogues with antimalarial activity: Design, synthesis and biological evaluation against Plasmodium falciparum parasites
ترجمه فارسی عنوان
آنالوگهای بورلیدین با فعالیت ضد مالاریا: طراحی، سنتز و ارزیابی بیولوژیکی علیه پارازیتهای پلاسمودیوم فالسیپاروم
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
Borrelidin, a structurally unique 18-membered macrolide, was found to express antimalarial activity against drug-resistant Plasmodium falciparum malaria parasites, with IC50 value of 0.93 ng/mL. However, it also displays strong cytotoxicity against human diploid embryonic MRC-5 cells. To investigate the issue of the cytotoxicity of borrelidin, borrelidin-based analogues were synthesized and their anti-Plasmodium properties were evaluated. In this communication, we report that a novel borrelidin analogue, bearing the CH2SPh moiety via a triazole linkage, was found to retain a potent antimalarial activity, against drug-sensitive and drug-resistant parasite strains, but possess only weak cytotoxicity against human cells.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 8, 15 April 2013, Pages 2302-2305
نویسندگان
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