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N-substituted bis-C-alkyloxadiazolones as dual effectors: efficient intermediates to amidoxines or amidines and prodrug candidates of potent antimalarials
Journal article   Open access   Peer reviewed

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

Melissa Degardin, Sharon Wein, Thierry Durand, R. Escale, Henri Vial and Yen Vo-Hoang
Bioorganic and Medicinal Chemistry Letters, Vol.19(17), pp.5233-5236
2009
DOI: https://doi.org/10.1016/j.bmcl.2009.07.001

Abstract

Bis-C-alkylamidine Convenient route N-substituted alkyloxadiazolone Alkylamidoxime Oral antimalarial agent Total clearance of parasitemia Design of prodrug candidates
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.
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