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Effect of ruthenium complexation on trypanocidal activity of 5-nitrofuryl containing thiosemicarbazones.
Pagano, Mariana; Demoro, Bruno; Toloza, Jeanette; Boiani, Lucía; González, Mercedes; Cerecetto, Hugo; Olea-Azar, Claudio; Norambuena, Ester; Gambino, Dinorah; Otero, Lucía.
Affiliation
  • Pagano M; Facultad de Química, Universidad de la República, Gral. Flores 2124, C.C. 1157, Montevideo 11800, Uruguay.
Eur J Med Chem ; 44(12): 4937-43, 2009 Dec.
Article in En | MEDLINE | ID: mdl-19783078
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 [RuCl(2)(HL)(2)], [RuCl(3)(dmso)(HL)] and [RuCl(PPh(3))(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.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Organometallic Compounds / Ruthenium / Thiosemicarbazones / Trypanocidal Agents / Nitrofurans Language: En Journal: Eur J Med Chem Year: 2009 Document type: Article Affiliation country: Uruguay Country of publication: France

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Organometallic Compounds / Ruthenium / Thiosemicarbazones / Trypanocidal Agents / Nitrofurans Language: En Journal: Eur J Med Chem Year: 2009 Document type: Article Affiliation country: Uruguay Country of publication: France