Synthesis of Antimalarial Bicyclic Hemiketal Peroxides Belonging to the G-factor Family
Synthesis of Antimalarial Bicyclic Hemiketal Peroxides Belonging to the G-factor Family作者机构：LSPCMIB UMR CNRS 5068 Universit~ Paul-Sabatier 118 route de Narbonne F-31062 Toulouse cedex 04 France CIRIMAT CNRS UMR 5085 ENSIACET 118 route de Narbonne 31077 Toulouse cedex 04 France LCP-SACS Universitd Aix-Marseille-CNRS UMR 6264 Campus St. Jdrome Case 512 13397 Marseille cedex 20 France LGC CNRS UMR 5503 Universitd Paul-Sabatier 118 route de Narbonne 31062 Toulouse France Department of Chemistry the University of Western Ontario London ON Canada N6A 5B7 Canada UMR CNRS 5539 Universitd Montpellier 2 cc107 Place E. Bataillon F-34095 Montpellier cedex 5 France
出 版 物：《Journal of Life Sciences》 (生命科学（英文版）)
年 卷 期：2010年第4卷第1期
页 面：38-42页
学科分类：090403[农学-农药学(可授农学、理学学位）] 08[工学] 09[农学] 0805[工学-材料科学与工程（可授工学、理学学位）] 080502[工学-材料学] 0904[农学-植物保护]
主 题：Antimalarial synthesis peroxide C-centered radical.
摘 要：Structural analogues of bicyclic peroxides belonging to the G factors family have been synthesised under Mannieh type conditions, followed by an autoxidation step furnishing exclusively the peroxide. As electron transfer from heine or free iron to peroxide is the first step in the mode of action ofartemisinin -like compound, Fe（fl） induced reduction was studied and the reactivity of the intermediate C-centered radical formed was correlated to the antimalarial activity. Dissociative electron transfer was studied by electrochemistry and allowed the evaluation of the standard reduction potentials and other pertinent thermochemical information. These bicyclic peroxides were evaluated in vitro against Plasmodium falciparum and revealed moderate to good activity.
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