Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity.
The reaction of thiosemicarbazones (TSCs) with [Au(I)(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.
Khanye
Setshaba D
SD
Department of Chemistry, University of Cape Town, Rondebosch, South Africa.
Smith
Gregory S
GS
Lategan
Carmen
C
Smith
Peter J
PJ
Gut
Jiri
J
Rosenthal
Philip J
PJ
Chibale
Kelly
K
D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003546:Cysteine Endopeptidases / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006046:Gold / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology / Q000254:growth & development; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013882:Thiosemicarbazones / Q000737:chemistry*
D000962:Antimalarials; D009942:Organometallic Compounds; D011480:Protease Inhibitors; D013882:Thiosemicarbazones; D006046:Gold; D003546:Cysteine Endopeptidases; C416224:falcipain 2