| Autor: |
Lima, Cintia M. C. F., Freitas Junior, Lúcio H., Moraes, Carolina B., Barbosa, Cecília G., Opatz, Till, Victor, Maurício M. |
| Jazyk: |
angličtina |
| Rok vydání: |
2023 |
| Předmět: |
|
| Zdroj: |
Journal of the Brazilian Chemical Society, Volume: 34, Issue: 5, Pages: 745-753, Published: 01 MAY 2023 |
| Popis: |
To expand the variety of density functionalized compounds evaluated against severe acute respiratory syndrome Coronavirus 2 (SARS-CoV-2), we decided to prepare new acetylated and disubstituted 3-hydroxy bis-oxindoles and isoindigos coupling compounds using known protocols. The corresponding isatin derivatives were synthesized by ZrCl4/EtOH/reflux or HCl/AcOH/reflux coupling conditions using oxindole and functionalized isatins, furnishing new 3-hydroxy bis-oxindoles, which were dehydrated into new isoindigos. A total of 27 compounds bearing halogen, nitro and/or hydroxy groups on the isatin moiety at the 3-, 5- and 7-positions, were prepared, including 5 new 3-hydroxy bis-oxindoles and 3 new halogenated isoindigos prepared according to adapted procedures described in the literature. This library of nitrogen-isatin derivatives was evaluated against SARS-CoV-2 using a phenotypic screening assay. In this investigation, isatin derivatives 3d, 3e, 3h and 3i showed antiviral activity when tested at a single concentration. Compound 3e showed antiviral activity against SARS-CoV-2 in the concentration-response assay; however, it showed cellular toxicity in Vero cells. The present study identified substituted isatins as a promising new starting point for the development of anti-SARS-CoV-2 agents. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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