1. Synthesis and antimalarial property of orally active phenoxazinium salts
- Author
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Tsubasa Shimogama, Marcel Kaiser, Kiyosei Takasu, Masataka Ihara, Chie Satoh, and Reto Brun
- Subjects
Plasmodium berghei ,education ,Plasmodium falciparum ,Drug Resistance ,Administration, Oral ,Parasitemia ,Pharmacology ,Lethal Dose 50 ,Antimalarials ,Mice ,Pharmacokinetics ,In vivo ,Oral administration ,parasitic diseases ,Drug Discovery ,Oxazines ,medicine ,Potency ,Animals ,biology ,Chemistry ,medicine.disease ,biology.organism_classification ,humanities ,Acute toxicity ,Bioavailability ,Malaria ,Quaternary Ammonium Compounds ,Molecular Medicine - 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-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.
- Published
- 2007