Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.

Detalhes bibliográficos
Autor(a) principal: Gomes, Paulo André Teixeira de Moraes
Data de Publicação: 2016
Outros Autores: Oliveira, Arsênio Rodrigues, Cardoso, Marcos Veríssimo de Oliveira, Santiago, Edna de Farias, Barbosa, Miria de Oliveira, Siqueira, Lucianna Rabelo Pessoa de, Moreira, Diogo Rodrigo Magalhães, Bastos, Tanira Matutino, Brayner, Fabio Andre, Soares, Milena Botelho Pereira, Oliveira Mendes, Andresa Pereira de, Castro, Maria Carolina Accioly Brelaz de, Pereira, Valeria Rego Alves, Leite, Ana Cristina Lima
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/14267
Resumo: Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil
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spelling Gomes, Paulo André Teixeira de MoraesOliveira, Arsênio RodriguesCardoso, Marcos Veríssimo de OliveiraSantiago, Edna de FariasBarbosa, Miria de OliveiraSiqueira, Lucianna Rabelo Pessoa deMoreira, Diogo Rodrigo MagalhãesBastos, Tanira MatutinoBrayner, Fabio AndreSoares, Milena Botelho PereiraOliveira Mendes, Andresa Pereira deCastro, Maria Carolina Accioly Brelaz dePereira, Valeria Rego AlvesLeite, Ana Cristina Lima2016-05-13T17:31:23Z2016-05-13T17:31:23Z2016GOMES, P. A. T. M. et al. Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi. European Journal of Medicinal Chemistry , v. 111, p.46-57, 2016.0223-5234https://www.arca.fiocruz.br/handle/icict/14267/dx.doi.org/10.1016/j.ejmech.2016.01.010engElsevierPhthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilLaboratório de Imunologia Keizo Asami-LIKA/UFPE. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Centro de Biotecnologia e Terapia Celular. Salvador BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilUniversidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, BrasilChagas disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affects approximately 6e7 million people worldwide. Benznidazole is the only drug approved for treatment during the acute and asymptomatic chronic phases; however, its efficacy during the symptomatic chronic phase is controversial. The present work reports the synthesis and anti-T. cruzi activities of a novel series of phthalimido-thiazoles. Some of these compounds showed potent inhibition of the trypomastigote form of the parasite at low cytotoxicity concentrations in spleen cells, and the resulting structure-activity relationships are discussed. We also showed that phthalimido-thiazoles induced ultrastructural alterations on morphology, flagellum shortening, chromatin condensation, mitochondria swelling, reservosomes alterations and endoplasmic reticulum dilation. Together, these data revealed, for the first time, a novel series of phthalimido-thiazoles-structure-based compounds with potential effects against T. cruzi and lead-like characteristics against Chagas disease.Chagas diseaseTrypanosoma cruziThiazoleHydrazonePhthalimideinfo: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/14267/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALGomes PATM Phthalimido....pdfGomes PATM Phthalimido....pdfapplication/pdf1703584https://www.arca.fiocruz.br/bitstream/icict/14267/2/Gomes%20PATM%20Phthalimido....pdf52e53fea525abd4a9ca1d384144f5738MD52TEXTGomes PATM Phthalimido....pdf.txtGomes PATM Phthalimido....pdf.txtExtracted 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dc.title.pt_BR.fl_str_mv Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
title Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
spellingShingle Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
Gomes, Paulo André Teixeira de Moraes
Chagas disease
Trypanosoma cruzi
Thiazole
Hydrazone
Phthalimide
title_short Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
title_full Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
title_fullStr Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
title_full_unstemmed Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
title_sort Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
author Gomes, Paulo André Teixeira de Moraes
author_facet Gomes, Paulo André Teixeira de Moraes
Oliveira, Arsênio Rodrigues
Cardoso, Marcos Veríssimo de Oliveira
Santiago, Edna de Farias
Barbosa, Miria de Oliveira
Siqueira, Lucianna Rabelo Pessoa de
Moreira, Diogo Rodrigo Magalhães
Bastos, Tanira Matutino
Brayner, Fabio Andre
Soares, Milena Botelho Pereira
Oliveira Mendes, Andresa Pereira de
Castro, Maria Carolina Accioly Brelaz de
Pereira, Valeria Rego Alves
Leite, Ana Cristina Lima
author_role author
author2 Oliveira, Arsênio Rodrigues
Cardoso, Marcos Veríssimo de Oliveira
Santiago, Edna de Farias
Barbosa, Miria de Oliveira
Siqueira, Lucianna Rabelo Pessoa de
Moreira, Diogo Rodrigo Magalhães
Bastos, Tanira Matutino
Brayner, Fabio Andre
Soares, Milena Botelho Pereira
Oliveira Mendes, Andresa Pereira de
Castro, Maria Carolina Accioly Brelaz de
Pereira, Valeria Rego Alves
Leite, Ana Cristina Lima
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Gomes, Paulo André Teixeira de Moraes
Oliveira, Arsênio Rodrigues
Cardoso, Marcos Veríssimo de Oliveira
Santiago, Edna de Farias
Barbosa, Miria de Oliveira
Siqueira, Lucianna Rabelo Pessoa de
Moreira, Diogo Rodrigo Magalhães
Bastos, Tanira Matutino
Brayner, Fabio Andre
Soares, Milena Botelho Pereira
Oliveira Mendes, Andresa Pereira de
Castro, Maria Carolina Accioly Brelaz de
Pereira, Valeria Rego Alves
Leite, Ana Cristina Lima
dc.subject.en.pt_BR.fl_str_mv Chagas disease
Trypanosoma cruzi
Thiazole
Hydrazone
Phthalimide
topic Chagas disease
Trypanosoma cruzi
Thiazole
Hydrazone
Phthalimide
description Universidade Federal de Pernambuco. Departamento de Ciências Farmacêuticas. Centro de Ciências da Saúde. Recife, PE, Brasil
publishDate 2016
dc.date.accessioned.fl_str_mv 2016-05-13T17:31:23Z
dc.date.available.fl_str_mv 2016-05-13T17:31:23Z
dc.date.issued.fl_str_mv 2016
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 GOMES, P. A. T. M. et al. Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi. European Journal of Medicinal Chemistry , v. 111, p.46-57, 2016.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/14267
dc.identifier.issn.none.fl_str_mv 0223-5234
dc.identifier.doi.none.fl_str_mv /dx.doi.org/10.1016/j.ejmech.2016.01.010
identifier_str_mv GOMES, P. A. T. M. et al. Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi. European Journal of Medicinal Chemistry , v. 111, p.46-57, 2016.
0223-5234
/dx.doi.org/10.1016/j.ejmech.2016.01.010
url https://www.arca.fiocruz.br/handle/icict/14267
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
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instacron:FIOCRUZ
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