Synthesis of 3,5-Diarylisoxazole derivatives and evaluation of in vitro trypanocidal activity.

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dc.contributor.authorSouza, Aline Aparecida Nunes de
dc.contributor.authorXavier, Viviane F.
dc.contributor.authorCoelho, Gleicekelly Silva
dc.contributor.authorSales Júnior, Policarpo Ademar
dc.contributor.authorRomanha, Alvaro José
dc.contributor.authorMurta, Silvane Maria Fonseca
dc.contributor.authorCarneiro, Claudia Martins
dc.contributor.authorTaylor, Jason Guy
dc.date.accessioned2018-03-13T15:38:11Z
dc.date.available2018-03-13T15:38:11Z
dc.date.issued2017
dc.description.abstractChagas 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 cruzi activity 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
dc.identifier.citationSOUZA, A. A. N. de et al. Synthesis of 3,5-Diarylisoxazole derivatives and evaluation of in vitro trypanocidal activity. Journal of The Brazilian Chemical Society, v. 28, n. 2, p. 269-277, 2017. Disponível em: <http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000200269>. Acesso em: 15 set. 2017.pt_BR
dc.identifier.doihttps://doi.org/10.21577/0103-5053.20170137
dc.identifier.issn1678-4790
dc.identifier.urihttp://www.repositorio.ufop.br/handle/123456789/9613
dc.language.isoen_USpt_BR
dc.rightsabertopt_BR
dc.rights.licenseJournal of the Brazilian Chemical Society permite que a UFOP deposite uma cópia em formato eletrônico dos artigos de seus alunos e professores publicados neste periódico no Repositório Institucional. Contato via email em 13 set. 2013.pt_BR
dc.subjectIsoxazolept_BR
dc.subjectTrypomastigotept_BR
dc.subjectAmastigotept_BR
dc.subjectAzolept_BR
dc.titleSynthesis of 3,5-Diarylisoxazole derivatives and evaluation of in vitro trypanocidal activity.pt_BR
dc.typeArtigo publicado em periodicopt_BR
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