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Increasing the Activity of copper(II) Complexes Against Leishmania Through Lipophilicity and Pro-Oxidant Ability

Increasing the Activity of copper(II) Complexes Against Leishmania Through Lipophilicity and Pro-Oxidant Ability

Andressa dos Santos Portas, Danilo Ciccone Miguel, Jenicer K U Yokoyama-Yasunaka, Silvia Reni Bortolin Uliana, Breno Pannia Espósito

J Biol Inorg Chem. 2012 Jan;17(1):107-12.

PMID: 21866394

Abstract:

Copper complexes with fluorinated β-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 necessary to improve selectivity of these compounds against the parasite.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP14324824	Copper(II) trifluoroacetylacetonate		14324-82-4	Price

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