title: The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi.
abstract: 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.
authors.affiliation: Departamento de Produtos Farmacêuticos, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
authors.forename: Marcela Silva
authors.initials: MS
authors.lastname: Lopes
authors.forename: Policarpo Ademar
authors.initials: PA
authors.lastname: Sales Júnior
authors.forename: Amanda Gervásio Ferreira
authors.initials: AG
authors.lastname: Lopes
authors.forename: Maria Irene
authors.initials: MI
authors.lastname: Yoshida
authors.forename: Thais Horta Alvares da
authors.initials: TH
authors.lastname: Silva
authors.forename: Alvaro José
authors.initials: AJ
authors.lastname: Romanha
authors.forename: Ricardo José
authors.initials: RJ
authors.lastname: Alves
authors.forename: Renata Barbosa de
authors.initials: RB
authors.lastname: Oliveira
mesh_terms: D007928:Lethal Dose 50; D008795:Metronidazole / Q000031:analogs & derivatives* / Q000494:pharmacology; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*; D047392:beta-Cyclodextrins / Q000494:pharmacology*
chemical_list: D014344:Trypanocidal Agents; D047392:beta-Cyclodextrins; D008795:Metronidazole