کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10591489 981754 2013 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Optimization of the electrophile of chloronitrobenzamide leads active against Trypanosoma brucei
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Optimization of the electrophile of chloronitrobenzamide leads active against Trypanosoma brucei
چکیده انگلیسی
We previously reported the phenylchloronitrobenzamides (PCNBs), a novel class of compounds active against the species of trypanosomes that cause Human African Trypanosomiasis (HAT). Herein, we explored the potential to adjust the reactivity of the electrophilic chloronitrobenzamide core. These studies identified compound 7d that potently inhibited the growth of trypanosomes (EC50 = 120 nM for Trypanosoma b. brucei, 18 nM for Trypanosoma b. rhodesiense, and 38 nM for Trypanosoma b. gambiense) without significant cytotoxicity against mammalian cell lines (EC50 > 25 μM for HepG2, HEK293, Raji, and BJ cell lines) and also had good stability in microsomal models (t1/2 > 4 h in both human and mouse). Overall these properties indicate the compound 7d and its analogs are worth further exploration as potential leads for HAT.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 14, 15 July 2013, Pages 4127-4131
نویسندگان
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