New artemisinin tricyclic analogs, bearing a methyl group at C-5a were
synthetized through ozonation of vinylsilanes. Presence of such a sub
stituent was detrimental to the antimalarial activity of these trioxan
es, thus reinforcing the hypothesis that tight hemin-trioxane complexe
s are involved in the activation phase of these compounds. (C) 1998 El
sevier Science Ltd. All rights reserved.