Orally active amino functionalized antimalarial 1,2,4-trioxanes

Bioorganic & Medicinal Chemistry Letters
2004.0

Abstract

Using readily available trioxanes 6a-b, a new series of amino functionalized 1,2,4-trioxanes 8a-e and 9a-e have been prepared and evaluated for antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice model. Several of these novel trioxanes are orally more active than the parent trioxanes 6a-b. Antimalarial activity of amino functionalized trioxane 9a, the most potent compound in the series, is very close to that of beta-arteether.

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