Probing Adamantane Arylhydroxamic Acids against <i>Trypanosoma brucei</i> and <i>Trypanosoma cruzi</i>
Angeliki Sofia Foscolos,
Andrew Tsotinis,
Martin C. Taylor,
John M. Kelly,
Ioannis P. Papanastasiou
Affiliations
Angeliki Sofia Foscolos
Division of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens Panepistimioupoli-Zografou, 15784 Athens, Greece
Andrew Tsotinis
Division of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens Panepistimioupoli-Zografou, 15784 Athens, Greece
Martin C. Taylor
Department of Infection Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1 E7HT, UK
John M. Kelly
Department of Infection Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1 E7HT, UK
Ioannis P. Papanastasiou
Division of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens Panepistimioupoli-Zografou, 15784 Athens, Greece
In this work, we present the synthesis and the anti-trypanosomal activity of the 2-(4-(adamant-1-yl)phenyl)-N-hydroxyarylamides, 1a,b and the 2-(4-(adamant-1-yl)phenoxy)-N-hydroxyacetamide, 1c. The 4-(adamant-1-yl)phenyl- and 4-(adamant-1-yl)phenoxy- moieties, which are endowed with promising drug-like properties, are functionalized at the side chain termini as hydroxamic acids. The phenoxy acetohydroxamic derivative, 1c, shows the most interesting profile in terms of activity and toxicity against trypanosomes and merits further investigation.
