abstract |
1,2,4-trioxolane diespirus and its methods of making and using a means and method of treating malaria, schistosomiasis, and cancer using a 1,2,4-trioxolane spiro or dyspirus is described. preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. in comparison with semi-synthetic artemisinin derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malaria parasites. the compounds of the invention surprisingly offer a single-dose cure for malaria, as well as prophylactic activity against it. the compounds are also active against schistosomiasis and cancer. |