New hydrazine and hydrazide quinoxaline 1,4-di- N -oxide derivatives: In silico ADMET, antiplasmodial and antileishmanial activity - Université Toulouse III - Paul Sabatier - Toulouse INP Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2017

New hydrazine and hydrazide quinoxaline 1,4-di- N -oxide derivatives: In silico ADMET, antiplasmodial and antileishmanial activity

Résumé

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 μM, FCR-3 IC50 = 2.56 μM) and 19 (3D7 IC50 = 0.24 μM, FCR-3 IC50 = 2.8 μM) were identified as the most active against P. falciparum, and they were the least cytotoxic (CC50-values > 241 μM) 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.
Fichier non déposé

Dates et versions

hal-03154943 , version 1 (01-03-2021)

Identifiants

Citer

Miguel Quiliano, Adriana Pabón, Gustavo Ramirez-Calderon, Carlos Barea, Eric Deharo, et al.. New hydrazine and hydrazide quinoxaline 1,4-di- N -oxide derivatives: In silico ADMET, antiplasmodial and antileishmanial activity. Bioorganic and Medicinal Chemistry Letters, 2017, 27 (8), pp.1820-1825. ⟨10.1016/j.bmcl.2017.02.049⟩. ⟨hal-03154943⟩
13 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More