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

• Main Authors: Marcela Silva Lopes, Policarpo Ademar Sales Júnior, Amanda Gervásio Ferreira Lopes, Maria Irene Yoshida, Thais Horta Alvares da Silva, Alvaro José Romanha, Ricardo José Alves, Renata Barbosa de Oliveira
• Format: Article
• Language: English
• Published: Instituto Oswaldo Cruz, Ministério da Saúde 2011-12-01
• Series: Memórias do Instituto Oswaldo Cruz.
• Subjects: nitroaromatic; cyclodextrin; Chagas disease; Trypanosoma cruzi
• Online Access: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000800027&lng=en&tlng=en

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.