In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi

Detalhes bibliográficos
Autor(a) principal: Salomão, K.
Data de Publicação: 2010
Outros Autores: Souza, E. M. de, Carvalho, S. A., Silva, E. F. da, Fraga, C. A. M., Barbosa, H. S., Castro, S. L. de
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/20911
Resumo: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
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spelling Salomão, K.Souza, E. M. deCarvalho, S. A.Silva, E. F. daFraga, C. A. M.Barbosa, H. S.Castro, S. L. de2017-09-05T12:39:39Z2017-09-05T12:39:39Z2010SALOMÃO, K. et al. In Vitro and In Vivo Activities of 1,3,4-Thiadiazole-2-Arylhydrazone Derivatives of Megazol against Trypanosoma cruzi. Antimicrobial Agents and Chmotherapy, v.54, n.5, p.2023-2031, May 2010.0066-4804https://www.arca.fiocruz.br/handle/icict/2091110.1128/AAC.01241-091098-6596engAntimicrobial Agents and ChemotherapyTrypanosoma cruziDoença de ChagasTécnicas In VitroMegazolTratamento1,3,4-Thiadiazole-2-ArylhydrazoneMegazolTrypanosoma cruziIn Vitro and In Vivo ActivitiesChagas diseaseIn vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruziinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Farmanguinhos. Departamento de Síntese Orgânica. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Farmanguinhos. Departamento de Síntese Orgânica. Rio de Janeiro, RJ. Brasil.Universidade Federal do Rio de Janeiro. Faculdade de Farmácia. Laboratório de Avaliação e Síntese de Substâncias Bioativas. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Estrutural. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.From a series of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol screened in vitro against Trypanosoma cruzi, eight (S1 to S8) were selected for in vivo screening by single-dose oral administration (200 mg/kg of body weight) to infected mice at 5 days postinfection (dpi). Based on significant decreases in both parasitemia levels and mortality rates, S2 and S3 were selected for further assays. Despite having no in vivo effect, S1 was included since it was 2-fold more potent against trypomastigotes than megazol in vitro. Trypomastigotes treated with S1, S2, or S3 showed alterations of the flagellar structure and of the nuclear envelope. When assayed on intracellular amastigotes, the selectivity index (SI) for macrophages was in the range of >27 to >63 and for cardiac cells was >32 for S1 and >48 for megazol. In noninfected mice, S1 did not alter the levels of glutamic oxalacetic transaminase (GOT), glutamate pyruvate transaminase (GPT), or urea. S2 led to an increase in GOT, S3 to increases in GOT and GPT, and megazol to an increase in GOT. Infected mice were treated with each derivative at 50 and 100 mg/kg from dpi 6 to 15: S1 did not interfere with the course of infection or reduce the number of inflammatory foci in the cardiac tissue, S2 led to a significant decrease of parasitemia, and S3 decreased mortality. There was no direct correlation between the in vitro effect on trypomastigotes and amastigotes and the results of the treatment in experimental models, as S1 showed a high potency in vitro while, in two different schemes of in vivo treatment, no decrease of parasitemia or mortality was observed.info: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/20911/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALk_salomao_etal_IOC_2010.pdfk_salomao_etal_IOC_2010.pdfapplication/pdf2061185https://www.arca.fiocruz.br/bitstream/icict/20911/2/k_salomao_etal_IOC_2010.pdf616d65ef433cbc9e5b08c98f8eaa67ffMD52TEXTk_salomao_etal_IOC_2010.pdf.txtk_salomao_etal_IOC_2010.pdf.txtExtracted 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dc.title.pt_BR.fl_str_mv In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
title In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
spellingShingle In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
Salomão, K.
Trypanosoma cruzi
Doença de Chagas
Técnicas In Vitro
Megazol
Tratamento
1,3,4-Thiadiazole-2-Arylhydrazone
Megazol
Trypanosoma cruzi
In Vitro and In Vivo Activities
Chagas disease
title_short In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
title_full In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
title_fullStr In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
title_full_unstemmed In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
title_sort In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi
author Salomão, K.
author_facet Salomão, K.
Souza, E. M. de
Carvalho, S. A.
Silva, E. F. da
Fraga, C. A. M.
Barbosa, H. S.
Castro, S. L. de
author_role author
author2 Souza, E. M. de
Carvalho, S. A.
Silva, E. F. da
Fraga, C. A. M.
Barbosa, H. S.
Castro, S. L. de
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Salomão, K.
Souza, E. M. de
Carvalho, S. A.
Silva, E. F. da
Fraga, C. A. M.
Barbosa, H. S.
Castro, S. L. de
dc.subject.other.pt_BR.fl_str_mv Trypanosoma cruzi
Doença de Chagas
Técnicas In Vitro
Megazol
Tratamento
topic Trypanosoma cruzi
Doença de Chagas
Técnicas In Vitro
Megazol
Tratamento
1,3,4-Thiadiazole-2-Arylhydrazone
Megazol
Trypanosoma cruzi
In Vitro and In Vivo Activities
Chagas disease
dc.subject.en.pt_BR.fl_str_mv 1,3,4-Thiadiazole-2-Arylhydrazone
Megazol
Trypanosoma cruzi
In Vitro and In Vivo Activities
Chagas disease
description Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil.
publishDate 2010
dc.date.issued.fl_str_mv 2010
dc.date.accessioned.fl_str_mv 2017-09-05T12:39:39Z
dc.date.available.fl_str_mv 2017-09-05T12:39:39Z
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 SALOMÃO, K. et al. In Vitro and In Vivo Activities of 1,3,4-Thiadiazole-2-Arylhydrazone Derivatives of Megazol against Trypanosoma cruzi. Antimicrobial Agents and Chmotherapy, v.54, n.5, p.2023-2031, May 2010.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/20911
dc.identifier.issn.pt_BR.fl_str_mv 0066-4804
dc.identifier.doi.none.fl_str_mv 10.1128/AAC.01241-09
dc.identifier.eissn.none.fl_str_mv 1098-6596
identifier_str_mv SALOMÃO, K. et al. In Vitro and In Vivo Activities of 1,3,4-Thiadiazole-2-Arylhydrazone Derivatives of Megazol against Trypanosoma cruzi. Antimicrobial Agents and Chmotherapy, v.54, n.5, p.2023-2031, May 2010.
0066-4804
10.1128/AAC.01241-09
1098-6596
url https://www.arca.fiocruz.br/handle/icict/20911
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 Antimicrobial Agents and Chemotherapy
publisher.none.fl_str_mv Antimicrobial Agents and Chemotherapy
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
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instacron_str FIOCRUZ
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collection Repositório Institucional da FIOCRUZ (ARCA)
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