Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives.
Amidoxime and O-substituted derivatives of the bis-alkylamidine 1,12-bis(N,N'-acetamidinyl)dodecane were synthesized and evaluated as in vitro and in vivo antimalarial prodrugs. The bis-O-methylsulfonylamidoxime 8 and the bis-oxadiazolone 9 derivatives show relatively potent antimalarial activity after oral administration.
Ouattara
Mahama
M
Dynamique Moléculaire des Interactions Membranaires, UMR 5539, CNRS-Université de Montpellier II, 34095 Montpellier, France.
Wein
Sharon
S
Calas
Michèle
M
Hoang
Yen Vo
YV
Vial
Henri
H
Escale
Roger
R
D000284:Administration, Oral; D000473:Alkanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D005260:Female; D006801:Humans; D006900:Hydroxylation; D007202:Indicators and Reagents; D007274:Injections, Intraperitoneal; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D016778:Malaria, Falciparum / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D016789:Plasmodium cynomolgi / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects
C518513:1,12-bis(N,N'-acetamidinyl)dodecane; D000473:Alkanes; D000578:Amidines; D000962:Antimalarials; D007202:Indicators and Reagents