Antimalarial t-butylperoxyamines.
Twelve t-butylperoxyamines (6-17) were synthesized as targeted antimalarials and evaluated for antimalarial activity in vivo against Plasmodium berghei in mice and in vitro against both chloroquine sensitive and chloroquine resistant strains of Plasmodium falciparum. Compound 8 was found to have highest potency with activity at 80 and 160mg/kg dose in vivo and compound 11 exhibited highest efficacy in vitro.
Sundar
N
N
Department of Chemistry, Indian Institute of Technology, Powai, Bombay 400 076, India.
Jacob
V T
VT
Bhat
S V
SV
Valecha
N
N
Biswas
S
S
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004352:Drug Resistance, Microbial; D016778:Malaria, Falciparum / Q000188:drug therapy; D051379:Mice; D009025:Morpholines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010545:Peroxides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects
C442368:4-(tert-butylperoxymethyl)morpholine; D000962:Antimalarials; D009025:Morpholines; D010545:Peroxides; D002738:Chloroquine