New readily accessible peroxides with high anti-malarial potency.
In an explorative study for new anti-malarial substances using the methyl esters (1 and 2) of peroxyplakoric acids A(3) and B(3) as scaffolds, 6-carbomethoxymethyl-3-methoxy-3-pentyl-1,2-dioxane, which has been readily synthesized from 6-keto-alpha,beta-unsaturated ester, was found to exhibit potent anti-malarial activity with high selective toxicity.
Murakami
Nobutoshi
N
Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, 565-0871, Osaka, Japan.
Kawanishi
Motoyuki
M
Itagaki
Sawako
S
Horii
Toshihiro
T
Kobayashi
Motomasa
M
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000494:pharmacology; D004146:Dioxanes / Q000138:chemical synthesis / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D010545:Peroxides / Q000138:chemical synthesis / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects; D011161:Porifera / Q000737:chemistry; D011422:Propionates / Q000138:chemical synthesis / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000962:Antimalarials; D004146:Dioxanes; D010545:Peroxides; D011422:Propionates; C093754:plakoric acid