Journal
POLYHEDRON
Volume 30, Issue 10, Pages 1718-1725Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.poly.2011.04.001
Keywords
Trypanosoma cruzi; Chagas disease; Chemotherapy; Fluoroquinolones; Metal complexes
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Funding
- Fiocruz
- Fundacao Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro [APQ1]
- Conselho Nacional Desenvolvimento cientifico e Tecnologico (CNPq)
- PDTIS/Fiocruz
- PAPES V/FIOCRUZ
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[MnCl2(NOR)(H2O)(2)] (1), [MnCl2(SPAR)(H2O)(2)] (2), [CoCl2(NOR)(H2O)(2)] (3) [CoCl2(SPAR)(H2O)(2)] (4), [CuCl2(phen)(NOR)] (5) and [CuCl2(phen)(SPAR)] (6) complexes with norfloxacin (NOR) and sparfloxacin (SPAR) were obtained from MnCl2 center dot 4H(2)O, CoCl2 center dot 4H(2)O and CuCl2(phen). In all cases the NOR and SPAR coordinate in the neutral zwitterionic form. The electron paramagnetic resonance spectra of the Cu(II) complexes (5) and (6) in aqueous and DMSO solutions indicate mixture of mononuclear and binuclear complex. Complexes (1-6), together with the corresponding ligands were evaluated for their in vitro trypanocidal effect, against both bloodstream trypomastigotes and intracellular forms of Trypanosoma SPAR and NOR were poorly effective upon T. cruzi, complexes (3) and (4) were active against intracellular forms of the parasite. The complexes (5) and (6) displayed a higher activity upon both bloodstream and intracellular forms. The potency of fluoroquinolones, specially those coordinated to Cu(II)-phen justify further trypanocidal screening assays with this compounds in vitro as well as upon experimental models of T. cruzi infection. (C) 2011 Elsevier Ltd. All rights reserved.
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