The activity of a metronidazole analogue and its beta-cyclodextrin complex against Trypanosoma cruzi

作者：Lopes Marcela Silva; Sales Junior Policarpo Ademar; Ferreira Lopes Amanda Gervasio; Yoshida Maria Irene; Alvares da Silva Thais Horta; Romanha Alvaro Jose; Alves Ricardo Jose; de Oliveira Renata Barbosa^*

来源：Memorias do Instituto Oswaldo Cruz, 2011, 106(8): 1055-1057.

DOI：10.1590/S0074-02762011000800027

• nitroaromatic
• cyclodextrin
• Chagas disease
• Trypanosoma cruzi

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:beta-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.

• 出版日期2011-12