Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity
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.
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Sociedade Brasileira de Química
2018
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oai:scielo:S0103-505320180002002692018-02-09Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal ActivitySouza,Aline A. N. deXavier,Viviane F.Coelho,Gleicekelly S.Sales Junior,Policarpo A.Romanha,Alvaro J.Murta,Silvane M. F.Carneiro,Claudia M.Taylor,Jason G. isoxazole azole amastigote trypomastigote in vitro Chagas disease 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.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society v.29 n.2 20182018-02-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000200269en10.21577/0103-5053.20170137 |
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Souza,Aline A. N. de Xavier,Viviane F. Coelho,Gleicekelly S. Sales Junior,Policarpo A. Romanha,Alvaro J. Murta,Silvane M. F. Carneiro,Claudia M. Taylor,Jason G. |
spellingShingle |
Souza,Aline A. N. de Xavier,Viviane F. Coelho,Gleicekelly S. Sales Junior,Policarpo A. Romanha,Alvaro J. Murta,Silvane M. F. Carneiro,Claudia M. Taylor,Jason G. Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity |
author_facet |
Souza,Aline A. N. de Xavier,Viviane F. Coelho,Gleicekelly S. Sales Junior,Policarpo A. Romanha,Alvaro J. Murta,Silvane M. F. Carneiro,Claudia M. Taylor,Jason G. |
author_sort |
Souza,Aline A. N. de |
title |
Synthesis of 3,5-Diarylisoxazole Derivatives and Evaluation of in vitro Trypanocidal Activity |
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 |
description |
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. |
publisher |
Sociedade Brasileira de Química |
publishDate |
2018 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000200269 |
work_keys_str_mv |
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