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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Optimization of the electrophile of chloronitrobenzamide leads active against Trypanosoma brucei Optimization of the electrophile of chloronitrobenzamide leads active against Trypanosoma brucei](/preview/png/10591489.png)
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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 14, 15 July 2013, Pages 4127-4131
نویسندگان
Jong Yeon Hwang, David C. Smithson, Gloria Holbrook, Fangyi Zhu, Michele C. Connelly, Marcel Kaiser, Reto Brun, R. Kiplin Guy,