Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents
| Autor(a) principal: | |
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| Data de Publicação: | 2017 |
| Outros Autores: | , , , , , , , , , , , , |
| 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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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. |
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2017 |
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2017-06-21T18:27:40Z |
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2017-06-21T18:27:40Z |
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2017 |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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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. |
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https://www.arca.fiocruz.br/handle/icict/19477 |
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1678-9946 |
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10.1590/S1678-9946201759008 |
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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 |
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https://www.arca.fiocruz.br/handle/icict/19477 |
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eng |
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