Synthesis of aminophenylhydroxamate and aminobenzylhydroxamate derivatives and in vitro screening for antiparasitic and histone deacetylase inhibitory activity

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 wa...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	International journal for parasitology -- drugs and drug resistance 2018-04, Vol.8 (1), p.59-66
Hauptverfasser:	Loeuillet, C., Touquet, B., Oury, B., Eddaikra, N., Pons, J.L., Guichou, J.F., Labesse, G., Sereno, D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiparasitic Agents - chemical synthesis Antiparasitic Agents - pharmacology Cell Line Chemical Sciences Dose-Response Relationship, Drug High-Throughput Screening Assays Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - isolation & purification Histone Deacetylase Inhibitors - pharmacology Histone Deacetylases - drug effects Humans Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Inhibitory Concentration 50 Leishmania - drug effects Life Sciences Medicinal Chemistry Microbiology and Parasitology Molecular Structure Parasitology Structure-Activity Relationship Toxoplasma - drug effects Trypanosoma - drug effects
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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 μM) that contrast with the highly efficient anti-Toxoplasma activity (IC50
ISSN:	2211-3207 2211-3207
DOI:	10.1016/j.ijpddr.2018.01.002