Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 82, Issue -, Pages 152-163Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.01.067
Keywords
Zinc(II) complexes; Nitrogen-based ligands; Valproic acid; Anti-bacterial activity; Anti-malarial activity; Hemozoin; beta-Hematin
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Funding
- office of Vice President for Academic Affairs at Birzeit University
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Starting from the precursor [Zinc Valproate complex] (1), new mixed ligand zinc(II) complexes of valproic acid and nitrogen-based ligands, formulating as, [Zn(valp)(2)2,9-dmphen] (2), [Zn-2(valp)(4)(quin)(2)] (3), [Zn(valp)(2)(2-ampy)(2)] (4), and [Zn(valp)(2)(2-ampic)(2)] (5) (valp = valproate, 2,9-dmphen = 2,9-dimethyl-1,10-phenanthroline, quin = quinoline, 2-ampy = 2-aminopyridine, 2-ampic = 2-amino-6-picoline) were synthesized and characterized using IR, H-1 NMR, C-13{H-1} NMR and UV-Vis spectrometry. The crystal structures of complexes 2, 3 and 4 were determined using single-crystal X-ray diffraction. The complexes were also evaluated for their anti-bacterial activity using in-vitro agar diffusion method against three Gram-positive (Micrococcus luteus, Staphylococcus aureus, and Bacillus subtilis) and three Gram-negative (Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis) species. Complex 2 showed considerable activity against all tested microorganisms and the effect of complexation on the anti-bacterial activity of the parent ligand of 2 was also investigated. The anti-bacterial activity of 2,9-dmphen against Gram-negative bacteria was enhanced upon complexation with zinc valproate. On the other hand, complexes 1 and 3 showed weak inhibition activity against the tested species and complexes 4 and 5 didn't show any activity at all. Two methods were used for testing the inhibition of ferriprotoporphyrinIX biomineralization: a semi-quantitative micro-assay and a previously self-developed quantitative in-vitro method. Both were used to study the efficiency of these complexes in inhibiting the formation of the Malaria pigment which considered being the target of many known anti-malarial drugs such as Chloroquine and Amodiaquine. Results showed that the efficiency of complex 2 in preventing the formation of beta-Hematin was 80%. The efficiency of Amodiaquine as a standard drug was reported to give 91%. (C) 2014 Elsevier Masson SAS. All rights reserved.
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