Athar, Fareeda, Husain, Kakul, Abid, Mohammad, Agarwal, Subhash M., Coles, Simon J., Hursthouse, Michael B., Maurya, Mannar R. and Azam, Amir (2005) Synthesis and anti-amoebic activity of gold(I), ruthenium(II), and copper(II) complexes of metronidazole. Chemistry & Biodiversity, 2 (10), 1320-1330. (doi:10.1002/cbdv.200590104).
Abstract
A series of Au, Ru, and Cu complexes of metronidazole (= [1-(2-hydroxyethyl)-2-methyl-5-nitro-1H-imidazole; 1) were prepared as highly potent anti-amoebic drugs. The complexes [Au(PPh3)(1)]PF6 (2), [Ru(1)(2)(Cl)2(H2O)2] (3), and [CU(1)(2)(mu-Cl)(H2O)](2)Cl-2 (4) were readily synthesized from [Au(PPh3)Cl], RuCl3·3H2O, and CuCl2·2H2O, respectively. All complexes were thoroughly characterized by IR, UV/VIS, H-1-NMR, FAB-MS, elemental and thermogravimetric analyses, and, in the case of 4, also by X-ray crystallography (Fig. 1). All complexes were evaluated in vitro as growth inhibitors of Entamoeba histolytica (HM1 : IMSS strain). Their IC50 values were in the range of 0.10 - 0.51 mu m (Table 2), which makes these drugs, especially the Cu-11 complex 4, considerably more potent than uncomplexed metronidazole (1: IC50 = 1.81 µM) the current standard drug for the worldwide treatment of amoebiasis.
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