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Eur J Med Chem ; 189: 112084, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-32000049

RESUMO

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.


Assuntos
Antiparasitários/farmacologia , Entamoeba histolytica/efeitos dos fármacos , Entamebíase/tratamento farmacológico , Compostos Organometálicos/farmacologia , Rutênio/química , Antiparasitários/química , Eletroquímica , Entamebíase/parasitologia , Compostos Organometálicos/química , Relação Estrutura-Atividade
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