title: Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives.
abstract: 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.
authors.affiliation: Dynamique Moléculaire des Interactions Membranaires, UMR 5539, CNRS-Université de Montpellier II, 34095 Montpellier, France.
authors.forename: Mahama
authors.initials: M
authors.lastname: Ouattara
authors.forename: Sharon
authors.initials: S
authors.lastname: Wein
authors.forename: Michèle
authors.initials: M
authors.lastname: Calas
authors.forename: Yen Vo
authors.initials: YV
authors.lastname: Hoang
authors.forename: Henri
authors.initials: H
authors.lastname: Vial
authors.forename: Roger
authors.initials: R
authors.lastname: Escale
mesh_terms: 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
chemical_list: C518513:1,12-bis(N,N'-acetamidinyl)dodecane; D000473:Alkanes; D000578:Amidines; D000962:Antimalarials; D007202:Indicators and Reagents