Pharmacodynamics and pharmacokinetics studies of phenoxazinium derivatives for antimalarial agent.
In vivo antimalarial drug candidates screening test was carried out on a series of water-soluble 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives. Among them, 3-(diethylamino)-7-(piperidin-1-yl)phenoxazin-5-ium chloride (SSJ-206) showing highest efficacy was chosen for further pharmcodynamics and pharmacokinetics study. It was supported from these data that the phenoxazinium salts, SSJ-206, would be one of hopeful candidates as an oral antimalarial drug.
Yang
Mei
M
Research Centre of Medicinal Sciences, Hoshi University, Shinagawa, Tokyo, Japan.
Ge
Jian-Feng
JF
Arai
Chika
C
Itoh
Isamu
I
Fu
Qiang
Q
Ihara
Masataka
M
D000818:Animals; D000962:Antimalarials / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology*; D005260:Female; D008288:Malaria / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010078:Oxazines / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
D000962:Antimalarials; D010078:Oxazines