Journal
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
Volume 27, Issue 6, Pages 1032-1039Publisher
SOC BRASILEIRA QUIMICA
DOI: 10.5935/0103-5053.20150360
Keywords
cyclopalladated; leishmaniasis; Chagas disease; Leishmania amazonensis; Trypanosoma cruzi; trypanosomiasis
Categories
Funding
- FAPESP (Fundacao de Amparo a Pesquisa do Estado de Sao Paulo) [201308248-1]
- CAPES (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior)
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The present study describes the antiprotozoal activities of four cyclopalladated compounds, [Pd(dmba)(mu-Cl)](2), [Pd(dmba)(NCO)(isn)], [Pd(dmba)(N-3)(isn)] and [Pd(dmba)(mu-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)(mu-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 mu M 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)(mu-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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