N-substituted bis-C-alkyloxadiazolones as dual effectors: Efficient intermediates to amidoximes or amidines and prodrug candidates of potent antimalarials

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.

Graphical abstractA convenient route to antimalarial N-substituted bis-C-alkylamidine drugs and their oxadiazolone and amidoxime prodrug candidates is described.Figure optionsDownload full-size imageDownload as PowerPoint slide