Author | Silva Júnior, Eufrânio N. da | |
Author | Souza, Maria Cecília B. V. de | |
Author | Fernandes, Michelle C. | |
Author | Menna-Barreto, Rubem F. S. | |
Author | Pinto, Maria do Carmo F. R. | |
Author | Lopes, Francisco de Assis | |
Author | Simone, Carlos Alberto de | |
Author | Andrade, Carlos Kleber Z. | |
Author | Pinto, Antônio V. | |
Author | Ferreira, Vitor F. | |
Author | Castro, Solange L. de | |
Access date | 2019-04-04T12:05:41Z | |
Available date | 2019-04-04T12:05:41Z | |
Document date | 2008 | |
Citation | SILVA JUNIOR, Eufrânio N. da Silva et al. Synthesis and anti-Trypanosoma cruzi activity of derivatives from nor-lapachones and lapachones. Bioorganic & Medicinal Chemistry, v. 16, n. 9, p. 5030–5038, Mar. 2008. | pt_BR |
ISSN | 0968-0896 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/32353 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | restricted access | pt_BR |
Subject in Portuguese | Doença de Chagas | pt_BR |
Subject in Portuguese | Atividade anti-Trypanosoma cruzi | pt_BR |
Subject in Portuguese | Síntese | pt_BR |
Subject in Portuguese | Lapachones | pt_BR |
Subject in Portuguese | Derivados de naftoquinona | pt_BR |
Title | Synthesis and anti-Trypanosoma cruzi activity of derivatives from nor-lapachones and lapachones | pt_BR |
Type | Article | pt_BR |
DOI | 10.1016/j.bmc.2008.03.032 | |
Abstract | New were synthesized and assayed against bloodstream trypomastigote forms of Trypanosoma cruzi, the etiological agent of Chagas' disease. The compounds were rationalized based on hybrid drugs and appear as important compounds against this parasite. From nor-lapachol were prepared five substituted ortho-naphthofuranquinones, a non-substituted para-naphthofuranquinone, a new oxyrane and an azide and from alpha-lapachone a new non-substituted para-naphthofuranquinone. Other five substituted ortho-naphthofuranquinones recently designed as cytotoxic, were also evaluated. The most active compounds were the ortho naphthofuranquinones 3-(4-methoxyphenylamino)-2,3-dihydro-2,2-dimethylnaphtho[1,2-b]furan-4,5-dione and 3-(3-nitrophenylamino)-2,3-dihydro-2,2-dimethylnaphtho[1,2-b]furan-4,5-dione with trypanocidal activity higher than that of benznidazole, the standard drug. The compounds were rationalized based on hybrid drugs and appear as important compounds against T. cruzi. The trypanocidal activity of these substances endowed with redox properties representing a good starting point for a medicinal chemistry program aiming the chemotherapy of Chagas' disease. | pt_BR |
Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil / Universidade de Brasília. Instituto de Química. Brasília, DF, Brasil. | pt_BR |
Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Núcleo de Pesquisas em Produtos Naturais. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Núcleo de Pesquisas em Produtos Naturais. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil. | pt_BR |
Affilliation | Universidade de Brasília. Instituto de Química. Brasília, DF, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Núcleo de Pesquisas em Produtos Naturais. Rio de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil. | pt_BR |
Subject | Chagas Disease | pt_BR |
Subject | Anti-Trypanosoma cruzi activity | pt_BR |
Subject | Synthesis | pt_BR |
Subject | Nor-lapachones | pt_BR |
Subject | Lapachones | pt_BR |
Subject | Naphthoquinone derivatives | pt_BR |
e-ISSN | 1464-3391 | |
Embargo date | 2022-01-01 | |