Synthesis and Antimalarial Property of Orally Active Phenoxazinium Salts

Journal of Medicinal Chemistry
2007.0

Abstract

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.

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