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
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 21, 1 November 2006, Pages 5682–5686
نویسندگان
Clare E. Gutteridge, Daniel A. Nichols, Sean M. Curtis, Darshan S. Thota, Joseph V. Vo, Lucia Gerena, Gettayacamin Montip, Constance O. Asher, Damaris S. Diaz, Charles A. DiTusa, Kirsten S. Smith, Apurba K. Bhattacharjee,