| Author | Gontijo, Talita B. | |
| Author | Carvalho, Renato L. de | |
| Author | Pereira, Luiza Dantas | |
| Author | Menna-Barreto, Rubem F. S. | |
| Author | Rogge, Torben | |
| Author | Ackermann, Lutz | |
| Author | Silva Júnior, Eufrânio N. da | |
| Access date | 2021-11-13T14:57:02Z | |
| Available date | 2021-11-13T14:57:02Z | |
| Document date | 2021 | |
| Citation | GONTIJO, Talita B. et al. Ruthenium(II)- and Palladium(II)-catalyzed position-divergent C–H oxygenations of arylated quinones: Identification of hydroxylated quinonoid compounds with potent trypanocidal activity. Bioorganic & Medicinal Chemistry, v. 40, 116164, p. 1 -11, Apr. 2021. | pt_BR |
| ISSN | 0968-0896 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/49829 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Quinones | pt_BR |
| Subject in Portuguese | Doença de Chagas | pt_BR |
| Subject in Portuguese | Rutênio | pt_BR |
| Subject in Portuguese | Paládio | pt_BR |
| Subject in Portuguese | Oxigenação C – H | pt_BR |
| Title | Ruthenium(II)- and Palladium(II)-catalyzed position-divergent C–H oxygenations of arylated quinones: Identification of hydroxylated quinonoid compounds with potent trypanocidal activity | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.bmc.2021.116164 | pt_BR |
| Abstract | against Trypanosoma cruzi, the etiological agent of Chagas disease, was accomplished. With the use of ruthenium
(II)- or palladium(II)-based catalysts, complementary regioselectivities were observed in the hydroxylation
reactions and we have identified 9 compounds more potent than benznidazole (Bz) among these novel arylated
and hydroxylated quinones. For instance, 5-hydroxy-2-[4-(trifluoromethyl)phenyl]-1,4-naphthoquinone (4h)
with an IC50/24 h value of 22.8 μM is 4.5-fold more active than the state-of-the-art drug Bz. This article provides
the first example of the application of C–H activation for the position-selective hydroxylation of arylated
quinones and the identification of these compounds as trypanocidal drug candidates. | pt_BR |
| Affilliation | Institut für Organische und Biomolekulare Chemie, Georg-August-Universitát Göttingen, Tammannstraße 2, 37077 Göttingen, Germany / Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Institut für Organische und Biomolekulare Chemie, Georg-August-Universitát Göttingen, Tammannstraße 2, 37077 Göttingen, Germany / Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. Belo Horizonte, MG, 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 | Institut für Organische und Biomolekulare Chemie, Georg-August-Universitát Göttingen, Tammannstraße 2, 37077 Göttingen, Germany. | pt_BR |
| Affilliation | Institut für Organische und Biomolekulare Chemie, Georg-August-Universitát Göttingen, Tammannstraße 2, 37077 Göttingen, Germany / DZHK (German Center for Cardiovascular Research), Potsdamer Strasse 58, 10785 Berlin, Germany. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais. Instituto de Ciências Exatas. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Subject | Quinones | pt_BR |
| Subject | Chagas Disease | pt_BR |
| Subject | Ruthenium | pt_BR |
| Subject | Palladium | pt_BR |
| Subject | C–H Oxygenation | pt_BR |
| DeCS | Rutênio | pt_BR |
| DeCS | Paládio | pt_BR |
| Embargo date | 2023 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
