New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2016 |
| 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/16525 |
Resumo: | CNPq; CAPES; PRONEX-FAPESB; PRONEM/FACEPE/CNPq. |
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Gomes, Paulo André Teixeira de MoraesBarbosa, Miria de OliveiraSantiago, Edna de FariasCardoso, Marcos Veríssimo de OliveiraCosta, Natáli Tereza CapistranoHernandes, Marcelo ZaldiniMoreira, Diogo Rodrigo MagalhãesSilva, Aline Caroline daSantos, Thiago André Ramos dosPereira, Valéria Rêgo AlvesSantos, Fábio André Brayner DosPereira, Glaécia Aparecida do NascimentoFerreira, Rafaela SalgadoLeite, Ana Cristina Lima2016-12-13T16:21:46Z2016-12-13T16:21:46Z2016GOMES, P. A. T. M. et al. New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi. European Journal of Medicinal Chemistry, v. 121, p. 387-398, 2016.0223-5234https://www.arca.fiocruz.br/handle/icict/1652510.1016/j.ejmech.2016.05.050CNPq; CAPES; PRONEX-FAPESB; PRONEM/FACEPE/CNPq.Universidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade de Pernambuco. Petrolina, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. 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, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilMinistry of Education of Brazil. CAPES Foundation. Brasília, DF, Brasil / Universidade Federal de Minas Gerais. Departamento de Bioquímica e Imunologia. Belo Horizonte, MG, BrasilUniversidade Federal de Minas Gerais. Departamento de Bioquímica e Imunologia. Belo Horizonte, MG, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilIn previous studies, the compound 3-(bromopropiophenone) thiosemicarbazone was described as a potent anti-Trypanosoma cruzi and cruzain inhibitor. In view to optimize this activity, 1,3-thiazole core was used as building-block strategy to access new lead generation of anti T. cruzi agents. In this way a series of thiazole derivatives were synthesized and most of these derivatives exhibited antiparasitic activity similar to benznidazole (Bzd). Among them, compounds (1c) and (1g) presented better selective index (SI) than Bzd. In addition, compounds showed inhibitory activity against the cruzain protease. As observed by electron microscopy, compound (1c) treatment caused irreversible and specific morphological changes on ultrastructure organization of T. cruzi, demonstrating that this class of compounds is killing parasites.engElsevierDoença de ChagasAgentes antiprotozoáriosTiazoleHidrazonasCruzainMicroscopia eletrônicaAntiprotozoal agentsChagas diseaseThiazoleHydrazonesCruzainElectron microscopyNew 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruziinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleinfo: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/16525/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALGomes PATM New 1,3-thiazole derivatives....pdfGomes PATM New 1,3-thiazole 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| dc.title.pt_BR.fl_str_mv |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| title |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| spellingShingle |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi Gomes, Paulo André Teixeira de Moraes Doença de Chagas Agentes antiprotozoários Tiazole Hidrazonas Cruzain Microscopia eletrônica Antiprotozoal agents Chagas disease Thiazole Hydrazones Cruzain Electron microscopy |
| title_short |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| title_full |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| title_fullStr |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| title_full_unstemmed |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| title_sort |
New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi |
| author |
Gomes, Paulo André Teixeira de Moraes |
| author_facet |
Gomes, Paulo André Teixeira de Moraes Barbosa, Miria de Oliveira Santiago, Edna de Farias Cardoso, Marcos Veríssimo de Oliveira Costa, Natáli Tereza Capistrano Hernandes, Marcelo Zaldini Moreira, Diogo Rodrigo Magalhães Silva, Aline Caroline da Santos, Thiago André Ramos dos Pereira, Valéria Rêgo Alves Santos, Fábio André Brayner Dos Pereira, Glaécia Aparecida do Nascimento Ferreira, Rafaela Salgado Leite, Ana Cristina Lima |
| author_role |
author |
| author2 |
Barbosa, Miria de Oliveira Santiago, Edna de Farias Cardoso, Marcos Veríssimo de Oliveira Costa, Natáli Tereza Capistrano Hernandes, Marcelo Zaldini Moreira, Diogo Rodrigo Magalhães Silva, Aline Caroline da Santos, Thiago André Ramos dos Pereira, Valéria Rêgo Alves Santos, Fábio André Brayner Dos Pereira, Glaécia Aparecida do Nascimento Ferreira, Rafaela Salgado 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 Barbosa, Miria de Oliveira Santiago, Edna de Farias Cardoso, Marcos Veríssimo de Oliveira Costa, Natáli Tereza Capistrano Hernandes, Marcelo Zaldini Moreira, Diogo Rodrigo Magalhães Silva, Aline Caroline da Santos, Thiago André Ramos dos Pereira, Valéria Rêgo Alves Santos, Fábio André Brayner Dos Pereira, Glaécia Aparecida do Nascimento Ferreira, Rafaela Salgado Leite, Ana Cristina Lima |
| dc.subject.other.pt_BR.fl_str_mv |
Doença de Chagas Agentes antiprotozoários Tiazole Hidrazonas Cruzain Microscopia eletrônica |
| topic |
Doença de Chagas Agentes antiprotozoários Tiazole Hidrazonas Cruzain Microscopia eletrônica Antiprotozoal agents Chagas disease Thiazole Hydrazones Cruzain Electron microscopy |
| dc.subject.en.pt_BR.fl_str_mv |
Antiprotozoal agents Chagas disease Thiazole Hydrazones Cruzain Electron microscopy |
| description |
CNPq; CAPES; PRONEX-FAPESB; PRONEM/FACEPE/CNPq. |
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2016 |
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2016-12-13T16:21:46Z |
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2016-12-13T16:21:46Z |
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2016 |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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article |
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publishedVersion |
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GOMES, P. A. T. M. et al. New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi. European Journal of Medicinal Chemistry, v. 121, p. 387-398, 2016. |
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https://www.arca.fiocruz.br/handle/icict/16525 |
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0223-5234 |
| dc.identifier.doi.none.fl_str_mv |
10.1016/j.ejmech.2016.05.050 |
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GOMES, P. A. T. M. et al. New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi. European Journal of Medicinal Chemistry, v. 121, p. 387-398, 2016. 0223-5234 10.1016/j.ejmech.2016.05.050 |
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Elsevier |
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Elsevier |
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