Synthesis and anti-amoebic activity of gold(I), ruthenium(II), and copper(II) complexes of metronidazole
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)
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Official URL: http://dx.doi.org/10.1002/cbdv.200590104
Description/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], RuCl(3)center dot 3H(2)O, and CuCl(2)center dot 2H(2)O, 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 mu M) the current standard drug for the worldwide treatment of amoebiasis.
| Item Type: | Article |
|---|---|
| ISSN: | 1612-1872 (print) |
| Uncontrolled Keywords: | entamoeba-histolytica, crystal-structure, in-vitro, coordination, derivatives, efficacy, agents, drugs, donor |
| Related URLs: | http://dx.doi.org/10.1002/cbdv.200590104 |
| Subjects: | Q Science > QD Chemistry |
| Divisions: | University Structure - Pre August 2011 > School of Chemistry |
| ePrint ID: | 20705 |
| URI: | http://eprints.soton.ac.uk/id/eprint/20705 |
| Deposited On: | 28 Feb 2006 |
| Last Modified: | 01 Jun 2011 09:36 |
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