کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369434 1379505 2016 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and activity of novel homodimers of Morita–Baylis–Hillman adducts against Leishmania donovani: A twin drug approach
ترجمه فارسی عنوان
سنتز و فعالیت های homodimers جدید مروری بیللی هیلمن در برابر لیشمانیا دونوانی: یک رویکرد دارویی دوقلو
کلمات کلیدی
ترکیب های موریتا-بایلیس-هیلمن؛ Homodimers؛ داروهای دوقلو؛ لیشمانیا دونووانی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

It is reported here the synthesis of novel Homodimers 12–19 of Morita–Baylis–Hillman adducts (MBHA) from one-pot Morita–Baylis–Hillman Reaction (MBHR) between aromatic aldehydes as eletrophiles and ethylene glycol diacrylate as Michael acceptor (35–94% yields) using cheap and green conditions. The bioactivities were evaluated against promastigote form of Leishmania donovani. All homodimers showed to be more potent than corresponding monomers. It is worth highlighting that the halogenated homodimers 17 and 18 (0.50 μM) is almost 400 times more active than the corresponding monomer 10 and 1.24 times more potent than the second-line drug amphotericin B (0.62 μM). Moreover, the selectivity index to 18 is very high (SIrb > 400) far better than amphotericin B (SIrb = 18.73). This is the first report of twin drugs strategy applied on Morita–Baylis–Hillman adducts.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 18, 15 September 2016, Pages 4523–4526
نویسندگان
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