Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity

Detalhes bibliográficos
Autor(a) principal: Souza, Aline Aparecida Nunes de
Data de Publicação: 2018
Outros Autores: Xavier, Viviane F., Coelho, Gleicekelly Silva, Sales Junior, Policarpo Ademar, Romanha, Alvaro José, Murta, Silvane Maria Fonseca, Carneiro, Claudia Martins, Taylor, Jason Guy
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/28763
Resumo: Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil
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spelling Souza, Aline Aparecida Nunes deXavier, Viviane F.Coelho, Gleicekelly SilvaSales Junior, Policarpo AdemarRomanha, Alvaro JoséMurta, Silvane Maria FonsecaCarneiro, Claudia MartinsTaylor, Jason Guy2018-09-13T18:12:29Z2018-09-13T18:12:29Z2018SOUZA, Aline A. N. de et al. Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity. J. Braz. Chem. Soc., v. 29, n. 2, p. 269-277, 20180103-5053https://www.arca.fiocruz.br/handle/icict/2876310.21577/0103-5053.20170137engSociedade Brasileira de Químicaisoxazolazoleamastigotetrypomastigotein vitroDoença de chagasisoxazoleazoleamastigotetrypomastigotein vitroChagas diseaseSynthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activityinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil/Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilFundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, BrazilFundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, BrazilFundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, BrazilUniversidade Federal de Ouro Preto. Núcleo de Pesquisas em Ciências Biológicas. Laboratório de Imunopatologia. Ouro Preto, MG, BrazilUniversidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, BrazilChagas disease is included in the neglected tropical diseases list and is endemic to 21 Latin American countries. The two drugs currently available for treating Chagas disease are nifurtimox and benznidazole and both result in many significant side effects. The study describes the synthesis and biological evaluation of 3,5-disubstituted isoxazoles. Isoxazoles were obtained by reaction of flavones and hydroxylamine and either alkylated at the free hydroxyl group and/or nitrated at the isoxazole ring. These compounds were evaluated for their in vitro anti-Trypanosoma cruziactivity against trypomastigote and amastigote forms of the parasite in T. cruzi-infected cell lineages. Benznidazole was used as a reference compound for the in vitro assay and mammalian L929 cells were employed to evaluate cytotoxicity. A majority of the compounds tested were very active and the most active isoxazole against amastigote and trypomastigotes of T. cruzi was slightly more potent than the current medicine benznidazole.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-83082https://www.arca.fiocruz.br/bitstream/icict/28763/1/license.txt9193a7c197bc67acd023525e72a03240MD51ORIGINALSynthesis of 3,5-Diarylisoxazole.pdfSynthesis of 3,5-Diarylisoxazole.pdfapplication/pdf3534631https://www.arca.fiocruz.br/bitstream/icict/28763/2/Synthesis%20of%203%2c5-Diarylisoxazole.pdf9500ac4aa901f6748a0175e3bc5cd308MD52TEXTSynthesis of 3,5-Diarylisoxazole.pdf.txtSynthesis of 3,5-Diarylisoxazole.pdf.txtExtracted texttext/plain333https://www.arca.fiocruz.br/bitstream/icict/28763/3/Synthesis%20of%203%2c5-Diarylisoxazole.pdf.txt46cbf89d5ee75b2812befaadbb7dbed3MD53icict/287632019-06-19 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dc.title.pt_BR.fl_str_mv Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
title Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
spellingShingle Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
Souza, Aline Aparecida Nunes de
isoxazol
azole
amastigote
trypomastigote
in vitro
Doença de chagas
isoxazole
azole
amastigote
trypomastigote
in vitro
Chagas disease
title_short Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
title_full Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
title_fullStr Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
title_full_unstemmed Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
title_sort Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
author Souza, Aline Aparecida Nunes de
author_facet Souza, Aline Aparecida Nunes de
Xavier, Viviane F.
Coelho, Gleicekelly Silva
Sales Junior, Policarpo Ademar
Romanha, Alvaro José
Murta, Silvane Maria Fonseca
Carneiro, Claudia Martins
Taylor, Jason Guy
author_role author
author2 Xavier, Viviane F.
Coelho, Gleicekelly Silva
Sales Junior, Policarpo Ademar
Romanha, Alvaro José
Murta, Silvane Maria Fonseca
Carneiro, Claudia Martins
Taylor, Jason Guy
author2_role author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Souza, Aline Aparecida Nunes de
Xavier, Viviane F.
Coelho, Gleicekelly Silva
Sales Junior, Policarpo Ademar
Romanha, Alvaro José
Murta, Silvane Maria Fonseca
Carneiro, Claudia Martins
Taylor, Jason Guy
dc.subject.other.pt_BR.fl_str_mv isoxazol
azole
amastigote
trypomastigote
in vitro
Doença de chagas
topic isoxazol
azole
amastigote
trypomastigote
in vitro
Doença de chagas
isoxazole
azole
amastigote
trypomastigote
in vitro
Chagas disease
dc.subject.en.pt_BR.fl_str_mv isoxazole
azole
amastigote
trypomastigote
in vitro
Chagas disease
description Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil
publishDate 2018
dc.date.accessioned.fl_str_mv 2018-09-13T18:12:29Z
dc.date.available.fl_str_mv 2018-09-13T18:12:29Z
dc.date.issued.fl_str_mv 2018
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 SOUZA, Aline A. N. de et al. Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity. J. Braz. Chem. Soc., v. 29, n. 2, p. 269-277, 2018
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/28763
dc.identifier.issn.pt_BR.fl_str_mv 0103-5053
dc.identifier.doi.none.fl_str_mv 10.21577/0103-5053.20170137
identifier_str_mv SOUZA, Aline A. N. de et al. Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity. J. Braz. Chem. Soc., v. 29, n. 2, p. 269-277, 2018
0103-5053
10.21577/0103-5053.20170137
url https://www.arca.fiocruz.br/handle/icict/28763
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 Sociedade Brasileira de Química
publisher.none.fl_str_mv Sociedade Brasileira de Química
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/28763/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/28763/2/Synthesis%20of%203%2c5-Diarylisoxazole.pdf
https://www.arca.fiocruz.br/bitstream/icict/28763/3/Synthesis%20of%203%2c5-Diarylisoxazole.pdf.txt
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