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

dc.creatorSouza, Aline Aparecida Nunes de
dc.creatorXavier, Viviane F.
dc.creatorCoelho, Gleicekelly Silva
dc.creatorSales Junior, Policarpo Ademar
dc.creatorRomanha, Alvaro José
dc.creatorMurta, Silvane Maria Fonseca
dc.creatorCarneiro, Claudia Martins
dc.creatorTaylor, Jason Guy
dc.date2018-09-13T18:12:29Z
dc.date2018-09-13T18:12:29Z
dc.date2018
dc.date.accessioned2023-09-26T20:22:35Z
dc.date.available2023-09-26T20:22:35Z
dc.identifierSOUZA, 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.identifier0103-5053
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/28763
dc.identifier10.21577/0103-5053.20170137
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8855496
dc.descriptionChagas 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.
dc.formatapplication/pdf
dc.languageeng
dc.publisherSociedade Brasileira de Química
dc.rightsopen access
dc.subjectisoxazol
dc.subjectazole
dc.subjectamastigote
dc.subjecttrypomastigote
dc.subjectin vitro
dc.subjectDoença de chagas
dc.subjectisoxazole
dc.subjectazole
dc.subjectamastigote
dc.subjecttrypomastigote
dc.subjectin vitro
dc.subjectChagas disease
dc.titleSynthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
dc.typeArticle


Este ítem pertenece a la siguiente institución