%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Quiliano, M.
%A Pabon, A.
%A Ramirez-Calderon, G.
%A Barea, C.
%A Deharo, Eric
%A Galiano, S.
%A Aldana, I.
%T New hydrazine and hydrazide quinoxaline 1,4-di-N-oxide derivatives : in silico ADMET, antiplasmodial and antileishmanial activity
%D 2017
%L fdi:010069519
%G ENG
%J Bioorganic and Medicinal Chemistry Letters
%@ 0960-894X
%K Malaria ; Leishmaniasis ; Quinoxaline 1,4-di-N-oxide ; Hydrazine ; Hydrazide
%M ISI:000399262600035
%N 8
%P 1820-1825
%R 10.1016/j.bmcl.2017.02.049
%U https://www.documentation.ird.fr/hor/fdi:010069519
%> https://www.documentation.ird.fr/intranet/publi/2017/05/010069519.pdf
%V 27
%W Horizon (IRD)
%X We report the design (in silico ADMET criteria), synthesis, cytotoxicity studies (HepG-2 cells), and biological evaluation of 15 hydrazine/hydrazide quinoxaline 1,4-di-N-oxide derivatives against the 3D7 chloroquine sensitive strain and FCR-3 multidrug resistant strain of Plasmodium falciparum and Leishmania infantum (axenic amastigotes). Fourteen of derivatives are novel quinoxaline 1,4-di-N-oxide derivatives. Compounds 18 (3D7 IC50 = 1.40 mu M, FCR-3 IC50 = 2.56 mu M) and 19 (3D7 IC50 = 0.24 mu M, FCR-3 IC50 = 2.8 mu M) were identified as the most active against P. falciparum, and they were the least cytotoxic (CC50-values > 241 mu M) and most selective (SI > 86). None of the compounds tested against L. infantum were considered to be active. Additionally, the functional role of the hydrazine and hydrazide structures were studied in the quinoxaline 1,4-di-N-oxide system.
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