Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
Keywords:
Schistosoma mansoni, Imidazolidines, UltrastructureAbstract
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.Downloads
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Published
2017-01-01
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Original Articles
How to Cite
Matos-Rocha, T. J., Lima, M. do C. A. de, Silva, A. L. da, Oliveira, J. F. de, Gouveia, A. L. A., Silva, V. B. R. da, Almeida Júnior, A. S. A. de, Brayner, F. A., Cardoso, P. R. G., Pitta-Galdino, M. da R., Pitta, I. da R., Rêgo, M. J. B. de M., Alves, L. C., & Pitta, M. G. da R. (2017). Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents. Revista Do Instituto De Medicina Tropical De São Paulo, 59, e8. https://revistas.usp.br/rimtsp/article/view/130562