title: Synthesis and antimalarial property of orally active phenoxazinium salts.
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.
authors: Kiyosei
authors: K
authors: Takasu
authors: Tsubasa
authors: T
authors: Shimogama
authors: Chie
authors: C
authors: Satoh
authors: Marcel
authors: M
authors: Kaiser
authors: Reto
authors: R
authors: Brun
authors: Masataka
authors: M
authors: Ihara
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004351:Drug Resistance; D007928:Lethal Dose 50; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010078:Oxazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D010078:Oxazines; D000644:Quaternary Ammonium Compounds