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Design and synthesis of amidoxime derivatives for orally potent C-alkylamidine-based antimalarial agents
Journal article   Peer reviewed

Design and synthesis of amidoxime derivatives for orally potent C-alkylamidine-based antimalarial agents

Mahama Ouattara, Sharon Wein, Séverine Denoyelle, Stéphanie Ortial, Thierry Durand, Roger Escale, Henri Vial and Yen Vo-Hoang
Bioorganic and Medicinal Chemistry Letters, Vol.19(3), pp.624-626
02/2009
DOI: https://doi.org/10.1016/j.bmcl.2008.12.058
PMID: 19124242

Abstract

C-Alkylamidine Design of prodrug Specific O-substitutions Alkylamidoxime Clearance of parasitemia Oral antimalarial agent Administration, Oral Animals Drug Design Humans Malaria Mice Models, Chemical Parasitemia Plasmodium falciparum Prodrugs Antimalarials Antioxidants Chemistry, Pharmaceutical Dose-Response Relationship, Drug
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.
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