کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1397084 | 1501228 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
High selective leishmanicidal activity of 3-hydroxy-2-methylene-3-(4-bromophenyl)propanenitrile and analogous compounds
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Sixteen not new aromatic compounds were prepared by one-pot reaction i.e. through Baylis–Hillman reaction and were the first time evaluated against promastigote Leishmania amazonensis and infected mammalian cells. Most of the compounds were selectively more active against amastigotes than the reference drug sodium stibogluconate (Pentostam, IC50 = 44.7 μM). We found that 3-hydroxy-2-methylene-3-(4-bromophenyl)propanenitrile (13) was the most active (IC50 = 12.5 μM) and safer compound (0.0 (0.9); % macrophage LDH release), being the lead compound.
We discovered a new class of Leishmanicide. These compounds are very efficient and selective against Leishmania amazonensis.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 42, Issue 1, January 2007, Pages 99–102
Journal: European Journal of Medicinal Chemistry - Volume 42, Issue 1, January 2007, Pages 99–102
نویسندگان
R.O.M.A. de Souza, V.L.P. Pereira, M.F. Muzitano, C.A.B. Falcão, B. Rossi-Bergmann, E.B.A. Filho, M.L.A.A. Vasconcellos,