Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes

[Display omitted] This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory conc...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2017-05, Vol.25 (10), p.2754-2760
Hauptverfasser: Rice, Douglas R., de Lourdes Betancourt Mendiola, María, Murillo-Solano, Claribel, Checkley, Lisa A., Ferdig, Michael T., Pizarro, Juan C., Smith, Bradley D.
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Sprache:eng
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Zusammenfassung:[Display omitted] This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600nM and almost no toxic effect against host cells including healthy red blood cells. Fluorescence microscopy studies with a green-fluorescent ZnDPA probe showed selective targeting of infected red blood cells. The results suggest that ZnDPA coordination complexes are promising antiplasmodial agents with potential for targeted malaria treatment.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2017.03.050