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Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents. 2017
Thiago José Matos-Rocha, and
Maria do Carmo Alves de Lima, and
Anekécia Lauro da Silva, and
Jamerson Ferreira de Oliveira, and
Allana Lemos Andrade Gouveia, and
Vinícius Barros Ribeiro da Silva, and
Antônio Sérgio Alves de Almeida, and
Fábio André Brayner, and
Pablo Ramon Gualberto Cardoso, and
Marina da Rocha Pitta-Galdino, and
Ivan da Rocha Pitta, and
Moacyr Jesus Barreto de Melo Rêgo, and
Luiz Carlos Alves, and
Maira Galdino da Rocha Pitta
Fundação Oswaldo Cruz (Fiocruz/PE), Centro de Pesquisas Aggeu Magalhães, Laboratório de Biologia Celular e Molecular, Recife, Pernambuco, Brazil.
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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