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

ABSTRACT: 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??M) that contrast with the highly efficient anti-Toxoplasma activity (IC50?

SUBMITTER: Loeuillet C

PROVIDER: S-EPMC6114082 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature

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

Loeuillet C C Touquet B B Oury B B Eddaikra N N Pons J L JL Guichou J F JF Labesse G G Sereno D D

International journal for parasitology. Drugs and drug resistance 20180131 1

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 (IC<sub>50</sub> > 10 μM) that contrast with the highly efficient anti-Toxoplasma activity (IC<sub>50</sub> < 1.0 μM) of these compounds. The antiparasitic activity of the synthetized compound ...[more]

PMID: 29414107

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