کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2487724 | 1114429 | 2007 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Ironâmediated degradation kinetics of substituted dispiroâ1,2,4âtrioxolane antimalarials
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The ironâmediated reactivity of various dispiroâ1,2,4âtrioxolanes was determined by automated kinetic analysis under standard reaction conditions. The active antimalarial compounds underwent peroxide bond cleavage by Fe(II) resulting in products indicative of carbonâcentered radical formation. The rate of reaction was heavily influenced by the presence of spiroâsubstituted adamantane and cyclohexane rings, and was also significantly affected by cyclohexane ring substitution. Steric hindrance around the peroxide oxygen atoms appeared to be the major determinant of reaction rate, however polar substituents also affected reactivity by an independent mechanism. A wide range of reaction rates was observed within this class of peroxide antimalarials, however ironâmediated reactivity did not directly correlate with in vitro antimalarial activity. © 2007 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 96: 2945-2956, 2007
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 96, Issue 11, November 2007, Pages 2945-2956
Journal: Journal of Pharmaceutical Sciences - Volume 96, Issue 11, November 2007, Pages 2945-2956
نویسندگان
Darren J. Creek, William N. Charman, Francis C.K. Chiu, Richard J. Prankerd, Kevin J. McCullough, Yuxiang Dong, Jonathan L. Vennerstrom, Susan A. Charman,