Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 12, Pages 4937-4943Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.08.008
Keywords
Chagas disease; Ruthenium complexes; 5-Nitrofuryl containing thiosemicarbazones
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Funding
- TWAS, Uruguay [02-036 RG/CHE/LA, ANII FCE 2007188]
- FONDECYT, Chile [1071068, 7070282]
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In the search of new therapeutic tools for the treatment of American Trypanosomiasis, the largest parasitic disease burden in the American continent, three series of novel ruthenium complexes of the formula [RuCl2(HL)(2)], [RuCl3(dmso)(HL)] and [RuCl(PPh3)(L)(2)] with bioactive 5-nitrofuryl containing thiosemicarbazones; as ligands (HL neutral, L monoanionic) were synthesized and characterized. Their in vitro growth inhibition activity against Trypanosoma cruzi and the effect of co-ligands in related physicochemical properties i.e. nitro moiety redox potential, lipophilicity and free radical scavenger capacity were evaluated. Results show that although a loss of activity was observed as a consequence of ruthenium complexation, lipophilicity and free radical scavenger capacity of the obtained complexes could be correlated to their trypanocidal effect. (C) 2009 Elsevier Masson SAS. All rights reserved.
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