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ited acceptable cytotoxicity of 19.9 mM. The Mn(II) complex
is about 2.4 times more active than sulfadiazine. Even
though the complexes are more toxic than sulfadiazine, they
are still less toxic than the widely used chloroquine
(IC50 ¼ 188.5 mM).[32] The Cu(II) and Mn(II) complexes are
candidates for further investigation.
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The complexes were also evaluated against axenic L.
donovani amastigotes and the T. b. rhodosiense tripomasti-
gotes. The studied stages are the most relevant clinically of
their life cycle. Against L. donovani, the Zn(II) and Mn(II)
complexes showed inhibition of growth at the micromolar
level with the manganese complex being the most potent.
The complexes of Cu(II), Pd(II), and Mn(II) inhibit the
growth of T. b. rhodosiense at the micromolar range. The
Cu(II) complex is the most potent and least toxic. At present,
2 compounds used to treat East African sleeping sickness are
very toxic. The early stage of T. b. rhodosiense disease is
treated with the nephrotoxic drugs suramin.[33] The other drug
in use is melarsoprol that has been restricted to the late-stage
of sleeping sickness because of its fatality. The Cu(II)
complex that is most active is less active than suramin
(IC50 ¼ 0.0075 mM)[34] and melarsoprol (IC50 ¼ 0.0039 mM).
These complexes still need to be optimized to make them
more soluble in DMSO and probably in water.
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CONCLUSION
Cu(II), Ni(II), Mn(II), Zn(II), Pd(II), and Pt(II) complexes
of sulfadiazine have been synthesised and characterised by
elemental analyses, electronic and IR spectra. All the com-
plexes are air stable and insoluble in most common solvents.
They have octahedral or square planar coordination in which
the metal ions are coordinated to sulfadiazine molecules that
act as bidentate ligands and some water molecules. The
Ni(II) complex contains two lattice water molecules. The in
vitro antiprotozoal screening on the complexes showed that
they have comparable activity like sulfadiazine except the
Mn(II) complexes that is more active in vitro than sulfadiazine.
They are generally more toxic than sulfadiazine but less toxic
than chloroquine.
14. Goldberg, D.; Sharma, E. V.; Oksman, A.; Gluzman, I. Y.;
Wellems, T. E.; Piwnica-Worms, D. Probing the locus of chloro-
quine resistance locus of Plasmodium falciparum with a Novel
class of multidentate metal (III) coordination complexes.
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