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Synthesis and Antimalarial Property of Orally Active Phenoxazinium Salts

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journal contribution
posted on 17.05.2007, 00:00 by Kiyosei Takasu, Tsubasa Shimogama, Chie Satoh, Marcel Kaiser, Reto Brun, Masataka Ihara
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-1 × 4 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.