| Author | Jardim, Guilherme A. M. | |
| Author | Silva, Thaissa L. | |
| Author | Goulart, Marilia O. F. | |
| Author | Simone, Carlos A. de | |
| Author | Barbosa, Juliana M. C. | |
| Author | Salomão, Kelly | |
| Author | Castro, Solange L. de | |
| Author | Bower, John F. | |
| Author | Silva Júnior, Eufrânio N. da | |
| Access date | 2017-11-09T16:33:24Z | |
| Available date | 2017-11-09T16:33:24Z | |
| Document date | 2017 | |
| Citation | JARDIM, Guilherme A. M. et al. Rhodium-catalyzed C-H bond activation for the synthesis of quinonoid compounds: Significant Anti-Trypanosoma cruzi activities and electrochemical studies of functionalized quinones. European Journal of Medicinal Chemistry, v.136, p.406-419, 2017. | pt_BR |
| ISSN | 0223-5234 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/23112 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Doença de Huntington | pt_BR |
| Subject in Portuguese | Trypanosoma cruzi | pt_BR |
| Subject in Portuguese | Quinonas | pt_BR |
| Subject in Portuguese | Eletroquímica | pt_BR |
| Title | Rhodium-catalyzed C-H bond activation for the synthesis of quinonoid compounds: Significant Anti-Trypanosoma cruzi activities and electrochemical studies of functionalized quinones | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.ejmech.2017.05.011 | |
| Abstract | Thirty four halogen and selenium-containing quinones, synthesized by rhodium-catalyzed C-H bond activation and palladium-catalyzed cross-coupling reactions, were evaluated against bloodstream trypomastigotes of T. cruzi. We have identified fifteen compounds with IC50/24 h values of less than 2 μM. Electrochemical studies on A-ring functionalized naphthoquinones were also performed aiming to correlate redox properties with trypanocidal activity. For instance, (E)-5-styryl-1,4-naphthoquinone 59 and 5,8-diiodo-1,4-naphthoquinone 3, which are around fifty fold more active than the standard drug benznidazole, are potential derivatives for further investigation. These compounds represent powerful new agents useful in Chagas disease therapy. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Alagoas. Instituto de Química e Biotecnologia. Maceió, AL, Brasil. | pt_BR |
| Affilliation | Universidade de São Paulo. Instituto de Física. Departamento de Física e Informática. São Carlos, SP, 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 | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ. Brasil. | pt_BR |
| Affilliation | University of Bristol. School of Chemistry. Bristol, UK. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Subject | C-H functionalization | pt_BR |
| Subject | Quinones | pt_BR |
| Subject | Chagas Disease | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Electrochemistry | pt_BR |
| e-ISSN | 1768-3254 | |
| Embargo date | 2030-01-01 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
