New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton.

[摘要]：The synthesis of the chimeric mols. consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes I, II, and III show relatively potent in vitro antimalarial activities, with IC90 values for the Plasmodium falciparum strain W2 of 2.26, 12.44, and 10.74 nM, resp. In addn., two compds., I and II, cured mice in a modified Thompson test for antimalarial blood stage activity, with a min. curative dose of 80 mg/kg, a min. active dose of 20 mg/kg/day, and a max. tolerated dose of >960 mg/kg.

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