title: N-substituted bis-C-alkyloxadiazolones as dual effectors: efficient intermediates to amidoximes or amidines and prodrug candidates of potent antimalarials.
abstract: A convenient route to N-substituted bis-C-alkylamidines possessing antiplasmodial activity and their oxadiazolone and amidoxime prodrug candidates, is described. These three families of compounds were available after a key N-alkylation step of the parent oxadiazolone 1a. Testing of the three compound classes in vitro and in vivo is also presented.
authors: Institut des Biomolécules Max Mousseron, UMR 5247, CNRS-Université Montpellier I, Université Montpellier II, Montpellier, France.
authors: Mélissa
authors: M
authors: Degardin
authors: Sharon
authors: S
authors: Wein
authors: Thierry
authors: T
authors: Durand
authors: Roger
authors: R
authors: Escale
authors: Henry
authors: H
authors: Vial
authors: Yen
authors: Y
authors: Vo-Hoang
mesh_terms: D000578:Amidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005260:Female; D051379:Mice; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010091:Oximes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010961:Plasmodium / Q000187:drug effects; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000578:Amidines; D000962:Antimalarials; D010069:Oxadiazoles; D010091:Oximes; D011355:Prodrugs