Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity
Journal of Inorganic Biochemistry
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Division of Pharmacology, University of Cape Town, Observatory 7925, South Africa; Department of Medicine, San Francisco General Hospital, University of California at San Francisco, CA 94143, United States; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa
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. © 2010 Elsevier Inc.
chloroquine; n [n (3 carboxyoxirane 2 carbonyl)leucyl]agmatine; tetrahydrothiophene derivative; antimalarial activity; article; in vitro study; infrared spectroscopy; mass spectrometry; microanalysis; nuclear magnetic resonance spectroscopy; synthesis; Antimalarials; Cysteine Endopeptidases; Dose-Response Relationship, Drug; Gold; Inhibitory Concentration 50; Models, Chemical; Molecular Structure; Organometallic Compounds; Plasmodium falciparum; Protease Inhibitors; Thiosemicarbazones; Plasmodium falciparum