| Author | Verzola, Marina Marina Mol Sena Andrade | |
| Author | Marques, Daisymara Priscila de Almeida | |
| Author | Silva, Elany Barbosa da | |
| Author | Serafim, Mateus Sá Magalhães | |
| Author | Ferreira, Rafaela Salgado | |
| Author | Fajtová, Pavla | |
| Author | Kohlhoff, Markus | |
| Author | O’Donoghue, Anthony John | |
| Author | Maltarollo, Vinícius Gonçalves | |
| Author | Reis, Jordana Grazziela Alves Coelho dos | |
| Author | Oliveira, Renata Barbosa de | |
| Access date | 2023-10-05T13:02:30Z | |
| Available date | 2023-10-05T13:02:30Z | |
| Document date | 2023 | |
| Citation | VERZOLA, Marina Mol Sena Andrade et al. Synthesis of indole-based ferulic acid derivatives and in vitro evaluation of antiviral activity against SARS-CoV-2. Medicinal Chemistry Research, v. 32, p. 2256–2267, 2023. https://doi.org/10.1007/s00044-023-03134-7. | en_US |
| ISSN | 1054-2523 | en_US |
| URI | https://www.arca.fiocruz.br/handle/icict/60713 | |
| Language | eng | en_US |
| Publisher | Springer | en_US |
| Rights | restricted access | |
| Title | Synthesis of indole-based ferulic acid derivatives and in vitro evaluation of antiviral activity against SARS-CoV-2. | en_US |
| Type | Article | |
| Abstract | The search for an effective small molecule against the severe acute respiratory syndrome related coronavirus 2 (SARS-CoV2) is a challenge that remains even after the end of the Coronavirus disease 2019 (COVID-19) global health emergency. The indole-based ferulic acid derivatives were synthesized in this work and evaluated for their in vitro cytotoxic profiles and antiSARS-CoV-2 activity. Compounds 1 and 2 decreased the number of genomic copies of SARS-CoV-2 in a dose-dependent manner, with IC50 values of 70.85 µM and 68.28 µM, respectively, with no significant cytotoxicity up to 100 µM against uninfected Vero cells. In order to search for a possible molecular target of these compounds, their activity against the two SARS-CoV-2 cysteine proteases, Mpro and PLpro, in addition to the human cysteine protease cathepsin L (hCatL) was investigated. However, they did not display significant activity against any of these proteases and, therefore, their mechanism of action remains unclear. Our findings suggest that the activity may be related to antioxidant properties of 1 and 2, since the presence of a phenolic group is critical for the antiviral activity. | en_US |
| Affilliation | Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA | en_US |
| Affilliation | Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil/Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA | en_US |
| Affilliation | Department of Biochemistry and Immunology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA | en_US |
| Affilliation | Chemistry of Natural Bioactive Products. René Rachou Institute. Oswaldo Cruz Foundation. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Skaggs School of Pharmacy and Pharmaceutical Sciences. University of California San Diego. La Jolla, CA, USA | en_US |
| Affilliation | Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Department of Microbiology. Institute of Biological Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil | en_US |
| Affilliation | Department of Pharmaceutical Products. Faculty of Pharmacy. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil | en_US |
| Subject | Antiviral activity | en_US |
| Subject | Coronavirus disease | en_US |
| Subject | Ferulic acid derivatives | en_US |
| Subject | Indole derivatives | en_US |
| Subject | SARS-CoV-2 | en_US |
| Embargo date | 3100-12-31 | |
