Journal
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
Volume 17, Issue 1, Pages 107-112Publisher
SPRINGER
DOI: 10.1007/s00775-011-0834-3
Keywords
Copper; Leishmaniasis; Lipophilicity; Dihydrorhodamine; Fluorescence
Funding
- CNPq (Brazilian government agency)
- FAPESP (Brazilian government agency)
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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 necessary to improve selectivity of these compounds against the parasite.
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