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New organoruthenium complexes with bioactive thiosemicarbazones as co-ligands: potential anti-trypanosomal agentsElectronic supplementary information (ESI) available. CCDC reference numbers 819342819343. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c1dt11519g

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-ligan...

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Main Authors: Demoro, Bruno, Sarniguet, Cynthia, Snchez-Delgado, Roberto, Rossi, Miriam, Liebowitz, Daniel, Caruso, Francesco, Olea-Azar, Claudio, Moreno, Virtudes, Medeiros, Andrea, Comini, Marcelo A, Otero, Luca, Gambino, Dinorah
Format: Article
Language:English
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Summary: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 [Ru 2 ( p -cymene) 2 (L) 2 ]X 2 , where X = Cl or PF 6 , 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. The prepared Ru complexes show in vitro activity against T. brucei brucei and potential for use as dual parasite inhibitors.
ISSN:1477-9226
1477-9234
DOI:10.1039/c1dt11519g