Synthesis, characterisation and in vitro studies of metal complexes of some selected antimalarial drugs
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Date
2005
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Publisher
University of Zululand
Abstract
This project deals with the synthesis, characterization and in vitro studies of metal complexes of antimalarial drugs. The synthetic techniques were based on the modification of antimalarial drugs by the introduction of metal ions into the molecular structure of the drugs. Thirty two metal complexes derived from chloroquine, amodiaquine, trimethoprim, sulfadiazine, tetracycline and pyrimethamine have been synthesised using the following metal ions: Co(II), Cu(II), Zn(II), Mn(II), Ni(II), Pt(II), Pd(II), Co(III), Fe(III), Ru(III) and VO(II). The complexes were characterised by melting point / decomposition temperature, solubility, conductivity measurement, elemental analyses, UV-Vis and IR spectroscopy, mass spectrometry, magnetic susceptibility measurement and EPR. Six of the complexes and sulfadiazine ligand were also characterised by single X-ray crystal studies.
The complexes were screened in vitro against four isolates of Plasmodium falciparum at various stages of the parasites development The results showed that three of the metal complexes, cobaIt(III)amodiaquine, cobalt(III)quinacrine and iron(III)amodiaquine are more active in vitro against the parasites in comparison to chloroquine the first drug of choice for treatment of chloroquine falciparum malaria in Africa.
Description
Thesis submitted in fulfilment of the requirement for the award of the degree of
Doctor of Philosophy in the Department of Chemistry at the University of Zululand, South Africa, 2005.
Keywords
Drugs--Physiological effect., Metal complexes--Evaluation., Antimalarials.