Increasing the activity of copper(II) complexes against Leishmania through lipophilicity and pro-oxidant ability

Portas, Andressa dos Santos
Miguel, Danilo Ciccone
Yasunaka, Jenicer Kazumi Umada Yokoyama
Uliana, Silvia Reni Bortolin
Esposito, Breno Pannia

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Publication date

January 2012

DOI

10.1007/s00775-011-0834-3

Publisher

NEW YORK

Journal

issn:0949-8257

Abstract

Copper complexes with fluorinated beta-diketones were synthesized and characterized in terms of lipophilicity and peroxide-assisted oxidation of dihydrorhodamine as an indicator of redox activity. The biological activity of the complexes was tested against promastigotes of Leishmania amazonensis. Inhibition of trypanosomatid-specific trypanothione reductase was also tested. It was found that the highly lipophilic and redox-active bis(trifluoroacetylacetonate) derivative had increased toxicity towards promastigotes. These results indicate that it is possible to modulate the activity of metallodrugs based on redox-active metals through the appropriate choice of lipophilic chelators in order to design new antileishmanials. Further work will be...