Increasing the activity of copper(II) complexes against Leishmania through lipophilicity and pro-oxidant ability
| Contribuinte(s) |
UNIVERSIDADE DE SÃO PAULO |
|---|---|
| Data(s) |
07/11/2013
07/11/2013
2012
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| Resumo |
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. CNPq (Brazilian government agency) Brazilian government agency CNPq Brazilian government agency FAPESP FAPESP (Brazilian government agency) |
| Identificador |
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY, NEW YORK, v. 17, n. 1, p. 107-112, JAN, 2012 0949-8257 http://www.producao.usp.br/handle/BDPI/43244 10.1007/s00775-011-0834-3 |
| Idioma(s) |
eng |
| Publicador |
SPRINGER NEW YORK |
| Relação |
Journal of Biological Inorganic Chemistry |
| Direitos |
closedAccess Copyright SPRINGER |
| Palavras-Chave | #COPPER #LEISHMANIASIS #LIPOPHILICITY #DIHYDRORHODAMINE #FLUORESCENCE #LABILE PLASMA IRON #TRYPANOTHIONE REDUCTASE #GLUTATHIONE-REDUCTASE #BIOLOGICAL-ACTIVITY #HYDROGEN-PEROXIDE #METABOLISM #DONOVANI #LIGANDS #NITRILOTRIACETATE #TRYPANOSOMATIDS #BIOCHEMISTRY & MOLECULAR BIOLOGY #CHEMISTRY, INORGANIC & NUCLEAR |
| Tipo |
article original article publishedVersion |
