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

Detalhes bibliográficos
Autor(a) principal: Matos-Rocha, Thiago José
Data de Publicação: 2017
Outros Autores: Lima, Maria do Carmo Alves de, Silva, Anekécia Lauro da, Oliveira, Jamerson Ferreira de, Gouveia, Allana Lemos Andrade, Silva, Vinícius Barros Ribeiro da, Almeida, 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
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/19477
Resumo: Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunomodulação e Novas Abordagens Terapêuticas. Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino. Recife, PE, Brasil.
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spelling Matos-Rocha, Thiago JoséLima, Maria do Carmo Alves deSilva, Anekécia Lauro daOliveira, Jamerson Ferreira deGouveia, Allana Lemos AndradeSilva, Vinícius Barros Ribeiro daAlmeida, Antônio Sérgio Alves deBrayner, Fábio AndréCardoso, Pablo Ramon GualbertoPitta-Galdino, Marina da RochaPitta, Ivan da RochaRêgo, Moacyr Jesus Barreto de MeloAlves, Luiz CarlosPitta, Maira Galdino da Rocha2017-06-21T18:27:40Z2017-06-21T18:27:40Z2017MATOS-ROCHA, T. J. et al. Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents. Revista do Instituto de Medicina Tropical de São Paulo, v. 59, n. 0, 2017.1678-9946https://www.arca.fiocruz.br/handle/icict/1947710.1590/S1678-9946201759008engSynthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agentsinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunomodulação e Novas Abordagens Terapêuticas. Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Imunomodulação e Novas Abordagens Terapêuticas. Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Planejamento e Síntese de Fármacos (LPSF). Departamento de Antibióticos. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Imunomodulação e Novas Abordagens Terapêuticas. Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino. Recife, PE, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Imunomodulação e Novas Abordagens Terapêuticas. Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino. Recife, PE, Brasil.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.Imidazolidinas / farmacologiaCélulas-Tronco de Sangue Periférico / efeitos de drogasSchistosoma mansoni / efeitos de drogasEsquistossomicidas / farmacologiainfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/19477/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINAL28380119 2017 roc-syn.oa.pdf28380119 2017 roc-syn.oa.pdfapplication/pdf851803https://www.arca.fiocruz.br/bitstream/icict/19477/2/28380119%202017%20roc-syn.oa.pdfff4e68b6cdfd9e17c9e231b727fbf9bbMD52TEXT28380119 2017 roc-syn.oa.pdf.txt28380119 2017 roc-syn.oa.pdf.txtExtracted 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dc.title.pt_BR.fl_str_mv Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
title Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
spellingShingle Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
Matos-Rocha, Thiago José
Imidazolidinas / farmacologia
Células-Tronco de Sangue Periférico / efeitos de drogas
Schistosoma mansoni / efeitos de drogas
Esquistossomicidas / farmacologia
title_short Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
title_full Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
title_fullStr Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
title_full_unstemmed Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
title_sort Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
author Matos-Rocha, Thiago José
author_facet 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, 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
author_role author
author2 Lima, Maria do Carmo Alves de
Silva, Anekécia Lauro da
Oliveira, Jamerson Ferreira de
Gouveia, Allana Lemos Andrade
Silva, Vinícius Barros Ribeiro da
Almeida, 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
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv 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, 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
dc.subject.decs.none.fl_str_mv Imidazolidinas / farmacologia
Células-Tronco de Sangue Periférico / efeitos de drogas
Schistosoma mansoni / efeitos de drogas
Esquistossomicidas / farmacologia
topic Imidazolidinas / farmacologia
Células-Tronco de Sangue Periférico / efeitos de drogas
Schistosoma mansoni / efeitos de drogas
Esquistossomicidas / farmacologia
description Fundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunomodulação e Novas Abordagens Terapêuticas. Núcleo de Pesquisas em Inovação Terapêutica Suely Galdino. Recife, PE, Brasil.
publishDate 2017
dc.date.accessioned.fl_str_mv 2017-06-21T18:27:40Z
dc.date.available.fl_str_mv 2017-06-21T18:27:40Z
dc.date.issued.fl_str_mv 2017
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv MATOS-ROCHA, T. J. et al. Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents. Revista do Instituto de Medicina Tropical de São Paulo, v. 59, n. 0, 2017.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/19477
dc.identifier.issn.pt_BR.fl_str_mv 1678-9946
dc.identifier.doi.pt_BR.fl_str_mv 10.1590/S1678-9946201759008
identifier_str_mv MATOS-ROCHA, T. J. et al. Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents. Revista do Instituto de Medicina Tropical de São Paulo, v. 59, n. 0, 2017.
1678-9946
10.1590/S1678-9946201759008
url https://www.arca.fiocruz.br/handle/icict/19477
dc.language.iso.fl_str_mv eng
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