Parasitic diseases such as malaria, African (sleeping sickness) and American (Chagas diseases) trypanosomiasis and leishmaniasis are common in tropical and subtropical regions of the world [1]. Multi-drug resistant strains of malaria parasites are becoming increasingly prevalent in the world [2]. The few drugs available for the treatment of African sleeping sickness and American Chagas diseases suffer from serious shortcomings [3-5]. In the search for new drugs against resistant parasitic protozoa's, the use of metal complexes has received attention [6-8]. In this study, the synthesis, characterization and in vitro antiplasmodial and antitrypanosomal activity of cobalt(III) and iron(III) complexes of amodiaquine and quinacrine are reported. The complexes were evaluated against axenic L. donovani amastigotes, T. cruzi amastigotes, T. b. rhodesience trypamastigotes and P. falciparum k1 strain. In vitro antiprotozoal studies of the complexes showed that the Co(III) and Fe(III) complexes of amodiaquine and quinacrine exhibited enhanced antitrypanosomal activities and the Co(III) complexes of amodiaquine and quinacrine and Fe(III) complex of amodiaquine are more active than chloroquine against the resistant strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) and less toxic.References 1. Schlapper, C., Seebacher, W., Faist, J., Kaizer, M., Brun, R., Saf, R., and Weis, R. Euro J . Med. Chem., 2009 , 44, 736.2. Tripathi, R.P., Mishra, R.C, Dwivedi, N., Tewari, N., and Verma, S.S. Curr. Med. Chem., 2005 , 12, 2643.3. Greenwood, B.M., Bojang, K., Whitty, C.J.M., and Targett, G.A.T. The Lancet, 2005 , 365, 1487.4. Wistanley, P.A., Ward, S.A., and Snow, R.W. Microbes Infect, 2002 , 4, 157.5. Barrett, M.P., Burchmore R.J.S., Stich, A., Lazzari, J.O., Frasch, A.C.,Cazzulo, J.J., and Krishna, S. Lancet, 2003 , 362, 1469.6. Navarro, M., Vasquez, F., Sanchez-Delgado, R.A., Perez, H., Sinou, V., and Sehrevel, J. J. Med. Chem., 2004 , 47(21), 5204.7. Ajibade, P.A., Kolawole, G.A. J. Coord. Chem. 2008 , 61, 3367.8. Ajibade, P.A., Kolawole, G.A. Synth. React. Inorg. Met.-Org. Nano-Met. Chem. 2010, 40, 273.

Cobalt(III) and Iron(III) complexes of antimalarial quinacrine and amodiaquine: Synthesis and in vitro antiprotozoal studies

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.