@article{fdi:010069519,
  title = {{N}ew hydrazine and hydrazide quinoxaline 1,4-di-{N}-oxide derivatives : in silico {ADMET}, antiplasmodial and antileishmanial activity},
  author = {{Q}uiliano, {M}. and {P}abon, {A}. and {R}amirez-{C}alderon, {G}. and {B}area, {C}. and {D}eharo, {E}ric and {G}aliano, {S}. and {A}ldana, {I}.},
  editor = {},
  language = {{ENG}},
  abstract = {{W}e report the design (in silico {ADMET} criteria), synthesis, cytotoxicity studies ({H}ep{G}-2 cells), and biological evaluation of 15 hydrazine/hydrazide quinoxaline 1,4-di-{N}-oxide derivatives against the 3{D}7 chloroquine sensitive strain and {FCR}-3 multidrug resistant strain of {P}lasmodium falciparum and {L}eishmania infantum (axenic amastigotes). {F}ourteen of derivatives are novel quinoxaline 1,4-di-{N}-oxide derivatives. {C}ompounds 18 (3{D}7 {IC}50 = 1.40 mu {M}, {FCR}-3 {IC}50 = 2.56 mu {M}) and 19 (3{D}7 {IC}50 = 0.24 mu {M}, {FCR}-3 {IC}50 = 2.8 mu {M}) were identified as the most active against {P}. falciparum, and they were the least cytotoxic ({CC}50-values > 241 mu {M}) and most selective ({SI} > 86). {N}one of the compounds tested against {L}. infantum were considered to be active. {A}dditionally, the functional role of the hydrazine and hydrazide structures were studied in the quinoxaline 1,4-di-{N}-oxide system.},
  keywords = {{M}alaria ; {L}eishmaniasis ; {Q}uinoxaline 1,4-di-{N}-oxide ; {H}ydrazine ; {H}ydrazide},
  booktitle = {},
  journal = {{B}ioorganic and {M}edicinal {C}hemistry {L}etters},
  volume = {27},
  numero = {8},
  pages = {1820--1825},
  ISSN = {0960-894{X}},
  year = {2017},
  DOI = {10.1016/j.bmcl.2017.02.049},
  URL = {https://www.documentation.ird.fr/hor/fdi:010069519},
}