title: Design and synthesis of amidoxime derivatives for orally potent C-alkylamidine-based antimalarial agents.
abstract: Within the frame of the design of prodrug candidates to deliver a C-alkylamidine antimalarial agent, we showed that specific O-substitutions were needed on the alkylamidoxime structure. Among the newly synthesized molecules, bis-oxadiazolone and bis-O-methylsulfonylamidoxime derivatives induced a complete clearance of parasitemia in mice after oral administration.
authors.affiliation: Institut des Biomolécules Max Mousseron, UMR 5247, CNRS - Université Montpellier I - Université Montpellier II, 34093 Montpellier, France.
authors.forename: Mahama
authors.initials: M
authors.lastname: Ouattara
authors.forename: Sharon
authors.initials: S
authors.lastname: Wein
authors.forename: Séverine
authors.initials: S
authors.lastname: Denoyelle
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Ortial
authors.forename: Thierry
authors.initials: T
authors.lastname: Durand
authors.forename: Roger
authors.initials: R
authors.lastname: Escale
authors.forename: Henri
authors.initials: H
authors.lastname: Vial
authors.forename: Yen
authors.initials: Y
authors.lastname: Vo-Hoang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D008956:Models, Chemical; D018512:Parasitemia / Q000188:drug therapy*; D010963:Plasmodium falciparum; D011355:Prodrugs
chemical_list: D000962:Antimalarials; D000975:Antioxidants; D011355:Prodrugs