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

Memórias do Instituto Oswaldo Cruz

Marcela Silva Lopes²  Policarpo Ademar Sales Júnior¹  Amanda Gervásio Ferreira Lopes²  Maria Irene Yoshida¹  Thais Horta Alvares Da Silva²  Alvaro José Romanha¹  Ricardo José Alves²  Renata Barbosa De Oliveira² 

[1] ,Universidade Federal de Minas Gerais Faculdade de Farmácia Departamento de Produtos FarmacêuticosBelo Horizonte MG ,Brasil

关键词: nitroaromatic;    cyclodextrin;    Chagas disease;    Trypanosoma cruzi;   

DOI  :  10.1590/S0074-02762011000800027

来源: SciELO

【 摘 要 】

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.

【 授权许可】

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