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The Synthesis, Characterization and Reactivity of a Series of Ruthenium N-triphosPh Complexes
Published on: April 10, 2015
Identification of descriptors for structure-activity relationship in ruthenium (II) mixed compounds with
Erika Lorena Cedillo-Gutiérrez1, Luis Felipe Hernández-Ayala1, Carolina Torres-Gutiérrez1
1Laboratorio de Química Inorgánica Medicinal, Facultad de Química Universidad Nacional Autónoma de México, Av. Universidad 3000, Circuito Exterior s/n, CU, P.O. Box 70-360, 04510, México City, Mexico.
Abstract:
Herein is presented the synthesis, characterization, electrochemical studies, DFT calculations and in vitro evaluation of amoebicidal activity in trophozoites of Entamoeba histolytica of twenty ruthenium (II) mixed compounds with general formulae: [Ru(pdto)(E-E)]Clx (E-E bidentate, either neutral or negatively charged ligands). For compounds under study, O-O, N-O and N-N auxiliary donor ligands demonstrate to have a crucial impact on the electronic properties and that it is possible to modulate the antiparasitic activity. Among analyzed complexes, only four present a better performance compared to typically used metronidazole drug (IC50 < 6.80 μmol/L) to treat amebiasis disease. For studied compounds, structure-activity relationships are strongly determined by either the redox potential (E1/2) of RuII/RuIII and calculated molar volume (V) of the complexes.
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