title: Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents.
abstract: 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.
authors.affiliation: Fundação Oswaldo Cruz (Fiocruz/PE), Centro de Pesquisas Aggeu Magalhães, Laboratório de Biologia Celular e Molecular, Recife, Pernambuco, Brazil.|Universidade Federal de Pernambuco, Laboratório de Imunopatologia Keizo Asami, Recife, Pernambuco, Brazil.|Universidade Federal de Pernambuco, Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino, Recife, Pernambuco, Brazil.
authors.forename: Thiago José
authors.initials: TJ
authors.lastname: Matos-Rocha
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Maria do Carmo Alves de
authors.initials: MD
authors.lastname: Lima
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Anekécia Lauro da
authors.initials: AL
authors.lastname: Silva
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Jamerson Ferreira de
authors.initials: JF
authors.lastname: Oliveira
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Allana Lemos Andrade
authors.initials: AL
authors.lastname: Gouveia
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Vinícius Barros Ribeiro da
authors.initials: VB
authors.lastname: Silva
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Antônio Sérgio Alves de
authors.initials: AS
authors.lastname: Almeida
authors.affiliation: Fundação Oswaldo Cruz (Fiocruz/PE), Centro de Pesquisas Aggeu Magalhães, Laboratório de Biologia Celular e Molecular, Recife, Pernambuco, Brazil.|Universidade Federal de Pernambuco, Laboratório de Imunopatologia Keizo Asami, Recife, Pernambuco, Brazil.
authors.forename: Fábio André
authors.initials: FA
authors.lastname: Brayner
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino, Recife, Pernambuco, Brazil.
authors.forename: Pablo Ramon Gualberto
authors.initials: PR
authors.lastname: Cardoso
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Marina da Rocha
authors.initials: MD
authors.lastname: Pitta-Galdino
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Planejamento e Síntese de Fármacos (LPSF), Departamento de Antibióticos, Recife, Pernambuco, Brazil.
authors.forename: Ivan da Rocha
authors.initials: ID
authors.lastname: Pitta
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino, Recife, Pernambuco, Brazil.
authors.forename: Moacyr Jesus Barreto de Melo
authors.initials: MJ
authors.lastname: Rêgo
authors.affiliation: Fundação Oswaldo Cruz (Fiocruz/PE), Centro de Pesquisas Aggeu Magalhães, Laboratório de Biologia Celular e Molecular, Recife, Pernambuco, Brazil.|Universidade Federal de Pernambuco, Laboratório de Imunopatologia Keizo Asami, Recife, Pernambuco, Brazil.
authors.forename: Luiz Carlos
authors.initials: LC
authors.lastname: Alves
authors.affiliation: Universidade Federal de Pernambuco, Laboratório de Imunomodulação e Novas Abordagens Terapêuticas, Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino, Recife, Pernambuco, Brazil.
authors.forename: Maira Galdino da Rocha
authors.initials: MG
authors.lastname: Pitta
mesh_terms: D000818:Animals; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D008855:Microscopy, Electron, Scanning; D021261:Parasitic Sensitivity Tests; D000072916:Peripheral Blood Stem Cells / Q000187:drug effects*; D012550:Schistosoma mansoni / Q000187:drug effects* / Q000648:ultrastructure; D012556:Schistosomicides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D013997:Time Factors
chemical_list: D048289:Imidazolidines; D012556:Schistosomicides