Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
The present study describes the antiprotozoal activities of four cyclopalladated compounds, [Pd(dmba)(μ-Cl)]2, [Pd(dmba)(NCO)(isn)], [Pd(dmba)(N3)(isn)] and [Pd(dmba)(μ-NCO)]2, (dmba: N,N'-dimethylbenzylamine and isn: isonicotinamide), against the diseases leishmaniasis (Leishmania amazonensis and Leishmania infantum), Chagas disease (Trypanosoma cruzi) and human African trypanosomiasis (Trypanosoma brucei). [Pd(dmba)(μ-NCO)]2 exhibited good leishmanicidal and trypanocidal activities against L. amazonensis and T. cruzi intracellular amastigote forms, with a 50% inhibitory concentration (IC50) value of less than 9 µM and selectivity indexes of 14.47 and 28.42, respectively. Stability essays were conducted in phosphate buffer saline (PBS) pH 7.0 and showed that [Pd(dmba)(μ-NCO)]2 is the most stable molecule. These findings indicate that this compound presented higher selectivity for these parasites than the other tested compounds. The data presented here suggest that this compound should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas disease.
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2016
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oai:scielo:S0103-505320160006010322016-06-21Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruziVelásquez,Angela M. A.Souza,Rodrigo A. dePassalacqua,Thaís G.Ribeiro,Aline R.Scontri,MateusChin,Chung M.Almeida,Leticia deCistia,Mayara L. DelRosa,João A. daMauro,Antonio E.Graminha,Marcia A. S. cyclopalladated leishmaniasis Chagas disease Leishmania amazonensis Trypanosoma cruzi trypanosomiasis The present study describes the antiprotozoal activities of four cyclopalladated compounds, [Pd(dmba)(μ-Cl)]2, [Pd(dmba)(NCO)(isn)], [Pd(dmba)(N3)(isn)] and [Pd(dmba)(μ-NCO)]2, (dmba: N,N'-dimethylbenzylamine and isn: isonicotinamide), against the diseases leishmaniasis (Leishmania amazonensis and Leishmania infantum), Chagas disease (Trypanosoma cruzi) and human African trypanosomiasis (Trypanosoma brucei). [Pd(dmba)(μ-NCO)]2 exhibited good leishmanicidal and trypanocidal activities against L. amazonensis and T. cruzi intracellular amastigote forms, with a 50% inhibitory concentration (IC50) value of less than 9 µM and selectivity indexes of 14.47 and 28.42, respectively. Stability essays were conducted in phosphate buffer saline (PBS) pH 7.0 and showed that [Pd(dmba)(μ-NCO)]2 is the most stable molecule. These findings indicate that this compound presented higher selectivity for these parasites than the other tested compounds. The data presented here suggest that this compound should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas disease.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society v.27 n.6 20162016-06-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532016000601032en10.5935/0103-5053.20150360 |
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Velásquez,Angela M. A. Souza,Rodrigo A. de Passalacqua,Thaís G. Ribeiro,Aline R. Scontri,Mateus Chin,Chung M. Almeida,Leticia de Cistia,Mayara L. Del Rosa,João A. da Mauro,Antonio E. Graminha,Marcia A. S. |
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Velásquez,Angela M. A. Souza,Rodrigo A. de Passalacqua,Thaís G. Ribeiro,Aline R. Scontri,Mateus Chin,Chung M. Almeida,Leticia de Cistia,Mayara L. Del Rosa,João A. da Mauro,Antonio E. Graminha,Marcia A. S. Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi |
author_facet |
Velásquez,Angela M. A. Souza,Rodrigo A. de Passalacqua,Thaís G. Ribeiro,Aline R. Scontri,Mateus Chin,Chung M. Almeida,Leticia de Cistia,Mayara L. Del Rosa,João A. da Mauro,Antonio E. Graminha,Marcia A. S. |
author_sort |
Velásquez,Angela M. A. |
title |
Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi |
title_short |
Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi |
title_full |
Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi |
title_fullStr |
Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi |
title_full_unstemmed |
Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi |
title_sort |
antiprotozoal activity of the cyclopalladated complexes against leishmania amazonensis and trypanosoma cruzi |
description |
The present study describes the antiprotozoal activities of four cyclopalladated compounds, [Pd(dmba)(μ-Cl)]2, [Pd(dmba)(NCO)(isn)], [Pd(dmba)(N3)(isn)] and [Pd(dmba)(μ-NCO)]2, (dmba: N,N'-dimethylbenzylamine and isn: isonicotinamide), against the diseases leishmaniasis (Leishmania amazonensis and Leishmania infantum), Chagas disease (Trypanosoma cruzi) and human African trypanosomiasis (Trypanosoma brucei). [Pd(dmba)(μ-NCO)]2 exhibited good leishmanicidal and trypanocidal activities against L. amazonensis and T. cruzi intracellular amastigote forms, with a 50% inhibitory concentration (IC50) value of less than 9 µM and selectivity indexes of 14.47 and 28.42, respectively. Stability essays were conducted in phosphate buffer saline (PBS) pH 7.0 and showed that [Pd(dmba)(μ-NCO)]2 is the most stable molecule. These findings indicate that this compound presented higher selectivity for these parasites than the other tested compounds. The data presented here suggest that this compound should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas disease. |
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Sociedade Brasileira de Química |
publishDate |
2016 |
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http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532016000601032 |
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