کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1376524 981959 2006 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vitro and in vivo efficacy and in vitro metabolism of 1-phenyl-3-aryl-2-propen-1-ones against Plasmodium falciparum
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
In vitro and in vivo efficacy and in vitro metabolism of 1-phenyl-3-aryl-2-propen-1-ones against Plasmodium falciparum
چکیده انگلیسی

Investigation of a series of 1-phenyl-3-aryl-2-propen-1-ones resulted in the identification of nine inhibitors with submicromolar efficacy against at least one Plasmodium falciparum strain in vitro. These inhibitors were inactive when given orally in a Plasmodium berghei infected mouse model. Significant compound degradation occurred upon their exposure to a liver microsome preparation, suggesting metabolic instability may be responsible for the lack of activity in vivo.

Nine in vitro submicromolar inhibitors of Plasmodium falciparum were identified, including compound 22. They were inactive when administered orally to Plasmodium berghei infected mice, possibly due to metabolic instability.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5682–5686
نویسندگان
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