Antimalarial activities of aminooxy compounds.
Twenty-three aminooxy compounds have been examined for their ability to inhibit the growth of the malaria parasite Plasmodium falciparum in vitro. Eight of these compounds were found to have 50% inhibitory concentrations less than 10 microM, with the best drugs being canaline (the aminooxy analogue of ornithine) and CGP51905A at 297 +/- 23.6 nM and 242 +/- 18.8 nM, respectively. Canaline was also assayed in combination with the ornithine decarboxylase inhibitor difluoromethylornithine, and the two drugs were found to be synergistic in antimalarial activity.
Berger
B J
BJ
Department of Biochemistry, University of Dundee, United Kingdom. bberger@dres.dnd.ca
D000613:Aminobutyrates / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004357:Drug Synergism; D000518:Eflornithine / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D006898:Hydroxylamines / Q000494:pharmacology*; D065108:Ornithine Decarboxylase Inhibitors; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development
D000613:Aminobutyrates; D000962:Antimalarials; C413416:CGP 51905A; D004791:Enzyme Inhibitors; D006898:Hydroxylamines; D065108:Ornithine Decarboxylase Inhibitors; C001926:canaline; D000518:Eflornithine