کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8994818 | 1114461 | 2005 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Kinetics of iron-mediated artemisinin degradation: Effect of solvent composition and iron salt
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
The antimalarial endoperoxides, such as artemisinin, are postulated to exert their potent parasiticidal activity via the formation of reactive intermediates in the iron-rich infected erythrocyte. The in vitro chemical reaction profile of putative endoperoxide antimalarials and ferrous iron is often qualitatively used to assess their potential antimalarial activity and to develop a structure-reactivity relationship. This study utilized LCMS to monitor the kinetics of artemisinin degradation and product formation in the presence of iron. A second order degradation reaction (k = 18 Mâ1 hâ1) was observed from the reaction of artemisinin with ferrous sulphate in aqueous acetonitrile to produce a number of stable isomeric rearrangement products. A systematic study of the effect of a number of solvent systems and different iron salts showed pronounced changes in reaction rate and product distribution. The significant effects observed in the current study highlight the need to carefully control reaction conditions when studying peroxide antimalarial stability or attempting to develop in vitro/in vivo correlations of endoperoxide antimalarials and their reactivity with iron.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 94, Issue 8, August 2005, Pages 1820-1829
Journal: Journal of Pharmaceutical Sciences - Volume 94, Issue 8, August 2005, Pages 1820-1829
نویسندگان
Darren J. Creek, Francis C.K. Chiu, Richard J. Prankerd, Susan A. Charman, William N. Charman,