The reactivity of 1, 2, 4-trioxane molecules 2-5, structurally related to the antimalarial drug artemisinin, with a heme model, manganese (II) tetraphenylporphyrin, is reported. With the pharmacologically active drugs 2-4, covalent adducts were obtained by addition of a drug- derived radical onto the porphyrin macrocycle, whereas no reaction was obtained with the nonactive compound 5. This confirms that alkylation is probably one of the key factors of ...
