Issue 5, 2012

New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: potential anti-trypanosomal agents

Abstract

In the search for new therapeutic tools against neglected diseases produced by trypanosomatid parasites, and particularly against African Trypanosomiasis, whose etiological agent is Trypanosoma brucei, organoruthenium compounds with bioactive nitrofuran containing thiosemicarbazones (L) as co-ligands were obtained. Four ruthenium(II) complexes with the formula [Ru2(p-cymene)2(L)2]X2, where X = Cl or PF6, were synthesized and the crystal structures of two of them were solved by X-ray diffraction methods. Two of the complexes show significant in vitro growth inhibition activity against Trypanosoma brucei brucei and are highly selective towards trypanosomal cells with respect to mammalian cells (J774 murine macrophages). These promising results make the title organoruthenium compounds good lead candidates for further developments towards potential antitrypanosomal organometallic drugs.

Graphical abstract: New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: potential anti-trypanosomal agents

Supplementary files

Article information

Article type
Paper
Submitted
11 Aug 2011
Accepted
31 Oct 2011
First published
02 Dec 2011

Dalton Trans., 2012,41, 1534-1543

New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: potential anti-trypanosomal agents

B. Demoro, C. Sarniguet, R. Sánchez-Delgado, M. Rossi, D. Liebowitz, F. Caruso, C. Olea-Azar, V. Moreno, A. Medeiros, M. A. Comini, L. Otero and D. Gambino, Dalton Trans., 2012, 41, 1534 DOI: 10.1039/C1DT11519G

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