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BIBTEX RIS

Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents

2017; UNIVERSIDADE DE SÃO PAULO; Volume: 59; Linguagem: Inglês

10.1590/s1678-9946201759008

ISSN

1678-9946

Autores

Thiago José Matos Rocha, Maria do Carmo Alves de Lima, Anekécia Lauro da Silva, Jamerson Ferreira de Oliveira, Allana Lemos Andrade Gouveia, Vinícius Barros Ribeiro da Silva, Antônio Sérgio Alves de Almeida Júnior, Fábio André Brayner, Pablo Ramon Gualberto Cardoso, Marina da Rocha Pitta-Galdino, Ivan da Rocha Pitta, Moacyr Jesus Barreto de Melo Rêgo, Luiz Carlos Alves, Maíra Galdino da Rocha Pitta,

Tópico(s)

Synthesis and biological activity

Resumo

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.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.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.The imidazolidine derivatives containing the trimetoxy and benzylidene halogens showed promising in vitro schistosomicidal activity.

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