| Author | Cardoso, Mariana F. do Carmo | |
| Author | Salomão, Kelly | |
| Author | Bombaça, Ana Cristina | |
| Author | Rocha, David R. da | |
| Author | Silva, Fernando de C. da | |
| Author | Cavaleiro, José A. S. | |
| Author | Castro, Solange L. de | |
| Author | Ferreira, Vitor F. | |
| Access date | 2016-05-17T13:13:59Z | |
| Available date | 2016-05-17T13:13:59Z | |
| Document date | 2015 | |
| Citation | CARDOSO, Mariana F. do Carmo; et al. Synthesis and anti-Trypanosoma cruzi activity of new 3-phenylthio-nor-b-lapachone derivatives. Bioorganic & Medicinal Chemistry, v.23, n.15, p.4763-4768, Aug. 2015. | pt_BR |
| ISSN | 0968-0896 | |
| URI | https://www.arca.fiocruz.br/handle/icict/14309 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | |
| Title | Synthesis and anti-Trypanosoma cruzi activity of new 3-phenylthio-nor-b-lapachone derivatives | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.bmc.2015.05.039 | |
| Abstract | We report herein a straightforward and efficient one-step reaction to prepare new nor-b-lapachone
derivatives tethered with phenylthio groups at position 3 of the furan ring. We have screened the compounds
on bloodstream trypomastigotes of Trypanosoma cruzi, the causative agent of Chagas disease,
aimed at finding a new prototype with high trypanocidal activity. The new compounds possess a broad
range of activity (IC50/24 h from 9.2 to 182.7 lM), higher than the original quinone (391.5 lM) and four of
them higher than standard drug benznidazole (103.6 lM). The most active was compound 13b (9.2 lM),
being 11 times active than benznidazole and the less toxic derivative to heart muscle cells. | 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 Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
| Affilliation | University of Aveiro. cDepartment of Chemistry and QOPNA. Aveiro, Portugal. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
| Subject | Naphthoquinone | pt_BR |
| Subject | Nor-b-lapachone | pt_BR |
| Subject | Thiol derivative | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Chagas Disease | pt_BR |
| DeCS | Doença de Chagas | pt_BR |
| DeCS | Trypanosoma cruzi | pt_BR |
| DeCS | Sulfidrila | pt_BR |
| e-ISSN | 1464-3391 | |
