Synthesis of 3,5-Diarylisoxazole derivatives and evaluation of in vitro trypanocidal activity.
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Date
2017
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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 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.
Description
Keywords
Isoxazole, Trypomastigote, Amastigote, Azole
Citation
SOUZA, 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.