Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
AUTOR(ES)
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 Júnior, 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
FONTE
Rev. Inst. Med. trop. S. Paulo
DATA DE PUBLICAÇÃO
03/04/2017
RESUMO
ABSTRACT 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.
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