Publications des scientifiques de l'IRD

Quiliano M., Pabon A., Ramirez-Calderon G., Barea C., Deharo Eric, Galiano S., Aldana I. (2017). New hydrazine and hydrazide quinoxaline 1,4-di-N-oxide derivatives : in silico ADMET, antiplasmodial and antileishmanial activity. Bioorganic and Medicinal Chemistry Letters, 27 (8), p. 1820-1825. ISSN 0960-894X.

Titre du document
New hydrazine and hydrazide quinoxaline 1,4-di-N-oxide derivatives : in silico ADMET, antiplasmodial and antileishmanial activity
Année de publication
2017
Type de document
Article référencé dans le Web of Science WOS:000399262600035
Auteurs
Quiliano M., Pabon A., Ramirez-Calderon G., Barea C., Deharo Eric, Galiano S., Aldana I.
Source
Bioorganic and Medicinal Chemistry Letters, 2017, 27 (8), p. 1820-1825 ISSN 0960-894X
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.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020] ; Santé : généralités [050] ; Entomologie médicale / Parasitologie / Virologie [052]
Localisation
Fonds IRD [F B010069519]
Identifiant IRD
fdi:010069519
Contact