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Mem. Inst. Oswaldo Cruz ; 106(8): 1055-1057, Dec. 2011. ilus, graf, tab
Artículo en Inglés | LILACS | ID: lil-610987

RESUMEN

In this study we prepared an inclusion complex between an iodide analogue of metronidazole (MTZ-I) and cyclodextrin (CD) to develop a safer and more effective method of treating Trypanosoma cruzi infections. According to our results, MTZ-I and MTZ-I:β-CD were 10 times more active than MTZ, demonstrating that the presence of an iodine atom on the side chain increased the trypanocidal activity while maintaining its cytotoxicity. The selective index shows that MTZ-I was 10 times more active against T. cruzi than it was against mammalian cells. The modification of MTZ side chains provides a promising avenue for the development of new drugs.


Asunto(s)
Metronidazol/análogos & derivados , Tripanocidas/farmacología , Trypanosoma cruzi/efectos de los fármacos , beta-Ciclodextrinas/farmacología , Metronidazol/farmacología , Pruebas de Sensibilidad Parasitaria , Relación Estructura-Actividad
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