| Author | Souza, Aline Aparecida Nunes de | |
| Author | Xavier, Viviane F. | |
| Author | Coelho, Gleicekelly Silva | |
| Author | Sales Junior, Policarpo Ademar | |
| Author | Romanha, Alvaro José | |
| Author | Murta, Silvane Maria Fonseca | |
| Author | Carneiro, Claudia Martins | |
| Author | Taylor, Jason Guy | |
| Access date | 2018-09-13T18:12:29Z | |
| Available date | 2018-09-13T18:12:29Z | |
| Document date | 2018 | |
| Citation | 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 | pt_BR |
| ISSN | 0103-5053 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/28763 | |
| Language | eng | pt_BR |
| Publisher | Sociedade Brasileira de Química | pt_BR |
| Rights | open access | pt_BR |
| Subject in Portuguese | isoxazol | pt_BR |
| Subject in Portuguese | azole | pt_BR |
| Subject in Portuguese | amastigote | pt_BR |
| Subject in Portuguese | trypomastigote | pt_BR |
| Subject in Portuguese | in vitro | pt_BR |
| Subject in Portuguese | Doença de chagas | pt_BR |
| Title | Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.21577/0103-5053.20170137 | |
| Abstract | Chagas 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. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
| Affilliation | Universidade 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, Brazil | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brazil | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Núcleo de Pesquisas em Ciências Biológicas. Laboratório de Imunopatologia. Ouro Preto, MG, Brazil | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Instituto de Ciências Exatas e Biológicas. Departamento de Química. Ouro Preto, MG, Brazil | pt_BR |
| Subject | isoxazole | pt_BR |
| Subject | azole | pt_BR |
| Subject | amastigote | pt_BR |
| Subject | trypomastigote | pt_BR |
| Subject | in vitro | pt_BR |
| Subject | Chagas disease | pt_BR |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
