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 trans...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.展开更多
文摘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.