American Trypanosomiasis and African Trypanosomiasis, diseases caused by Trypanosoma cruzi and Trypanosoma brucei respectively, constitute major health concerns in the developing world. Based on the recognition of common targets in both parasites, drugs active against both protozoa could offer an innovative approach for anti-parasitic drug discovery. During the last years we have successfully developed potential anti-T. cruzi agents by metal coordination of trypanocidal ligands.  Metal-drug combined effects could lead to enhance  ligands� activity and to generate new mechanisms of action. In this presentation, efforts to develop anti-trypanosomal ruthenium complexes with bioactive 5-nitrofuryl thiosemicarbazones as ligands are discussed. In particular, organoruthenium complexes show to be highly selective T. cruzi and T. brucei growth inhibitors. The interaction of the most active derivatives with serum proteins was characterized by circular dichroism and fluorescence spectroscopy in simulated blood plasma conditions. Additionally, attempts to get insight into their mechanism of action are described.

Ruthenium complexes as promising hits for the design of potential agents against multiple trypanosomatid parasites

243rd National Meeting (2012)

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