1188302-69-3Relevant articles and documents
Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: Relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity
Wang, Xiaofang,Creek, Darren J.,Schiaffo, Charles E.,Dong, Yuxiang,Chollet, Jacques,Scheurer, Christian,Wittlin, Sergio,Charman, Susan A.,Dussault, Patrick H.,Wood, James K.,Vennerstrom, Jonathan L.
, p. 4542 - 4545 (2009)
These data suggest that iron(II) reactivity for a set of homologous spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane peroxide heterocycles is a necessary, but insufficient, property of animalarial peroxides. Heme alkylation efficiency appears to give a more accurate prediction of antimalarial activity than FeSO4-mediated reaction rates, suggesting that antimalarial activity is not merely dependent on peroxide bond cleavage, but also on the ability of reactive intermediates to alkylate heme or other proximal targets.