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Loeuillet C., Touquet B., Oury Bruno, Eddaikra N., Pons J. L., Guichou J. F., Labesse G., Sereno Denis. (2018). Synthesis of aminophenylhydroxamate and aminobenzylhydroxamate derivatives and in vitro screening for antiparasitic and histone deacetylase inhibitory activity. International Journal for Parasitology : Drugs and Drug Resistance, 8 (1), p. 59-66. ISSN 2211-3207.

Titre du document
Synthesis of aminophenylhydroxamate and aminobenzylhydroxamate derivatives and in vitro screening for antiparasitic and histone deacetylase inhibitory activity
Année de publication
2018
Type de document
Article référencé dans le Web of Science WOS:000428405000008
Auteurs
Loeuillet C., Touquet B., Oury Bruno, Eddaikra N., Pons J. L., Guichou J. F., Labesse G., Sereno Denis
Source
International Journal for Parasitology : Drugs and Drug Resistance, 2018, 8 (1), p. 59-66 ISSN 2211-3207
A series of aminophenylhydroxamates and aminobenzylhydroxamates were synthesized and screened for their antiparasitic activity against Leishmania, Trypanosoma, and Toxoplasma. Their anti-histone deacetylase (HDAC) potency was determined. Moderate to no antileishmanial or antitrypanosomal activity was found (IC50 > 10 mu M) that contrast with the highly efficient anti-Toxoplasma activity (IC50 < 1.0 mu M) of these compounds. The antiparasitic activity of the synthetized compounds correlates well with their HDAC inhibitory activity. The best-performing compound (named 363) express a high anti-HDAC6 inhibitory activity (IC50 of 0.045 +/- 0.015 mu M) a moderate cytotoxicity and a high anti-Toxoplasma activity in the range of known anti-Toxoplasma compounds (IC50 of 0.35-2.25 mu M). The 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-Toxoplasma molecules.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020] ; Entomologie médicale / Parasitologie / Virologie [052]
Localisation
Fonds IRD [F B010072672]
Identifiant IRD
fdi:010072672
Contact