Phenoxazinium salts were found to display good antimalarial efficacy in vivo against Plasmodium berghei. Several compounds provided 100% parasitemia clearance at a dose of 20-30 mg kg-1x4 days (ip) and good survival effects without obvious acute toxicity. They also showed excellent potency by oral administration. A preliminary pharmacokinetic study revealed that the oral availability of 1a was excellent.

Phenoxazinium salts show good antimalarial efficacy and excellent oral availability, with potential for use in malaria treatment without acute toxicity.

Paper

Synthesis and antimalarial property of orally active phenoxazinium salts.

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