@article{fdi:010072672,
  title = {{S}ynthesis of aminophenylhydroxamate and aminobenzylhydroxamate derivatives and in vitro screening for antiparasitic and histone deacetylase inhibitory activity},
  author = {{L}oeuillet, {C}. and {T}ouquet, {B}. and {O}ury, {B}runo and {E}ddaikra, {N}. and {P}ons, {J}. {L}. and {G}uichou, {J}. {F}. and {L}abesse, {G}. and {S}ereno, {D}enis},
  editor = {},
  language = {{ENG}},
  abstract = {{A} series of aminophenylhydroxamates and aminobenzylhydroxamates were synthesized and screened for their antiparasitic activity against {L}eishmania, {T}rypanosoma, and {T}oxoplasma. {T}heir anti-histone deacetylase ({HDAC}) potency was determined. {M}oderate to no antileishmanial or antitrypanosomal activity was found ({IC}50 > 10 mu {M}) that contrast with the highly efficient anti-{T}oxoplasma activity ({IC}50 < 1.0 mu {M}) of these compounds. {T}he antiparasitic activity of the synthetized compounds correlates well with their {HDAC} inhibitory activity. {T}he best-performing compound (named 363) express a high anti-{HDAC}6 inhibitory activity ({IC}50 of 0.045 +/- 0.015 mu {M}) a moderate cytotoxicity and a high anti-{T}oxoplasma activity in the range of known anti-{T}oxoplasma compounds ({IC}50 of 0.35-2.25 mu {M}). {T}he calculated selectivity index (10-300 using different human cell lines) of the compound 363 makes it a lead compound for the future development of anti-{T}oxoplasma molecules.},
  keywords = {},
  booktitle = {},
  journal = {{I}nternational {J}ournal for {P}arasitology : {D}rugs and {D}rug {R}esistance},
  volume = {8},
  numero = {1},
  pages = {59--66},
  ISSN = {2211-3207},
  year = {2018},
  DOI = {10.1016/j.ijpddr.2018.01.002},
  URL = {https://www.documentation.ird.fr/hor/fdi:010072672},
}