Spiro and dispiro 1,2,4-trioxolane antimalarials

Details Spiro and dispiro 1,2,4-trioxolane antimalarials Spiro and dispiro 1,2,4-trioxolane antimalarials

C - Chemistry, Metallurgy

07

D

C07D 323/02 (2006.01) A61K 31/357 (2006.01) A61K 31/4525 (2006.01) A61K 31/496 (2006.01) A61P 33/06 (2006.01) A61P 33/12 (2006.01) C07D 405/08 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2478146

A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The 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, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non- toxic, and potent against malarial parasites.

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