Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity

The reaction of thiosemicarbazones (TSCs) with [AuI(THT)Cl], THT = tetrahydrothiophene, has been investigated. The resulting gold(I) complexes have been characterized by a range of spectroscopic techniques: NMR spectroscopy, mass spectrometry, microanalysis and infrared spectroscopy. The in vitro antimalarial data for gold(I) TSC complexes suggests that coordination of gold(I) to TSCs enhanced their efficacy against the malaria parasite Plasmodium falciparum and their inhibition of the parasite cysteine protease falcipain-2.

The synthesis and characterization of gold(I) compounds of the type [Au(HLn)2]+.CI−, wher HLn = thiosemicarbazones, n = 1−7, are described. In vitro biological evaluation of these thiosemicarbazone revealed enhanced antiplasmodial activity and inhibition of the malarial cysteine protease falcipain−2 compared to the free ligands.Figure optionsDownload as PowerPoint slide