Article
Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
Registro en:
MATOS-ROCHA, T. J. et al. Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents. Revista do Instituto de Medicina Tropical de São Paulo, v. 59, n. 0, 2017.
1678-9946
10.1590/S1678-9946201759008
Autor
Matos-Rocha, Thiago José
Lima, Maria do Carmo Alves de
Silva, Anekécia Lauro da
Oliveira, Jamerson Ferreira de
Gouveia, Allana Lemos Andrade
Silva, Vinícius Barros Ribeiro da
Almeida, Antônio Sérgio Alves de
Brayner, Fábio André
Cardoso, Pablo Ramon Gualberto
Pitta-Galdino, Marina da Rocha
Pitta, Ivan da Rocha
Rêgo, Moacyr Jesus Barreto de Melo
Alves, Luiz Carlos
Pitta, Maira Galdino da Rocha
Resumen
INTRODUCTION::
Schistosomiasis is an infectious parasitic disease caused by trematodes of the genus Schistosoma, which threatens at least 258 million people worldwide and its control is dependent on a single drug, praziquantel. The aim of this study was to evaluate the anti-Schistosoma mansoni activity in vitro of novel imidazolidine derivatives.
MATERIAL AND METHODS: :
We synthesized two novel imidazolidine derivatives: (LPSF/PTS10) (Z)-1-(2-chloro-6-fluorobenzyl)-4-(4-dimethylaminobenzylidene)-5-thioxoimidazolidin-2-one and (LPSF/PTS23) (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one. The structures of two compounds were determined by spectroscopic methods. During the biological assays, parameters such as motility, oviposition, mortality and analysis by Scanning Electron Microscopy were performed.
RESULTS: :
LPSF/PTS10 and LPSF/PTS23 were considered to be active in the separation of coupled pairs, mortality and to decrease the motor activity. In addition, LPSF/PTS23 induced ultrastructural alterations in worms, after 24 h of contact, causing extensive erosion over the entire body of the worms.
CONCLUSION: :
The imidazolidine derivatives containing the trimetoxy and benzylidene halogens showed promising in vitro schistosomicidal activity.