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Eur J Med Chem ; 98: 54-60, 2015 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-26005916

RESUMEN

Two promising palladium(II) compounds of general formula, cis-[Pd(L-O,S)2] [where HL-O,S = N-(di(butyl/phenyl)carbamothioyl)benzamide] as metal based antiamoebic drug candidates, have been synthesized. Both complexes are characterized in the solid state by FT-IR spectroscopy, TGA and single crystal X-ray study, as well as in solution by other spectroscopic techniques such as (1)H and (13)C NMR, and UV-visible. All these studies confirm the coordination of ligands through oxygen and sulphur atoms upon thioenolization induced delocalization. Complexes adopt cis-configuration in the solid state. Both the complexes and their respective ligands were screened in vitro for antiamoebic activity against HM1:1MSS strain of Entamoeba histolytica by microdilution method and cell viability in response to drugs was checked by using MTT assay. The IC50 values in the range 0.30-0.80 µM for ligands as well as complexes compared to 1.40 for metronidazole along with their similar inhibitory effect on cell viability of HEK293 cells like metronidazole make them promising future antiamoebic drugs.


Asunto(s)
Amebicidas/química , Amebicidas/farmacología , Benzamidas/química , Benzamidas/farmacología , Complejos de Coordinación/química , Complejos de Coordinación/farmacología , Paladio/química , Feniltiourea/análogos & derivados , Evaluación Preclínica de Medicamentos , Entamoeba histolytica/efectos de los fármacos , Concentración 50 Inhibidora , Modelos Moleculares , Feniltiourea/química , Feniltiourea/farmacología
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