Metal complexes of drugs used as ligands

Sadler etal.18 used bis-tetraazamacrocyclo-xylyl-bicyclan, shown in Figure 21.4, a potent anti-HIV (human immunodeficiency virus) agent, to prepare a series of metal complexes with Zn(II) and Pd(II), and tried to achieve recognition by the co-receptor CXCR4, a G-protein coupled receptor used by the HIV for membrane fusion and cell entry. While Zn(II)2-xylyl-bicyclam complexes give indications of binding to CXCR4, involving the carboxylate groups Asp262 (Zn(II) coordination), the corresponding square planar Pd(II) complexes interact only weakly with axial ligands and are thus inactive.

Complexes of Pd(II) and Pt(II) with metronidazole, a highly effective drug of formula [M(mnz)2Cl2] (against the acute disease caused by E. histolytica), were found more active than the free drug against the same disease (IC50 0.103 mM for the Pd(II) analogue vs 1.50 mM).19

Two complexes of Pd(II) with diphenylpyraline (DPH) and isothipendyl (IPH), showing anti-serotonin, -histaminic, -convulsant and -fungal activity, of formulae [Pd(DPH)2Cl2] and [Pd(IPH)Cl2], were synthesized and studied for their anti-bacterial and -fungal activities against Alternaria alternata, A. tenius, Aspergillus flavus, A. niger, Staphylococcus aureus and E. coli. Their antimicrobial activity was higher than that of the free ligands.20

The anti-viral activity of Pd(II) complexes with the anti-herpic drug pen-ciclovir (pen) of formulae cis-[(pen)2PdCl2] and cis-[(nucl)2Pd(pen)2]Cl2 (nucl = guanosine, inosine, cytidine or penciclovir) were tested. All prepared complexes were markedly active against HIV-1 and HSV-2 (herpes simplex virus) strains but not against the thymidine kinase-deficient HSV-1 strain in E6SM diploid fibroblastic cell cultures.21

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