| Autor: |
Silvia Cesarini, Ilaria Vicenti, Federica Poggialini, Massimiliano Secchi, Federica Giammarino, Ilenia Varasi, Camilla Lodola, Maurizio Zazzi, Elena Dreassi, Giovanni Maga, Lorenzo Botta, Raffaele Saladino |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Molecules, Vol 27, Iss 24, p 8829 (2022) |
| Druh dokumentu: |
article |
| ISSN: |
1420-3049 |
| DOI: |
10.3390/molecules27248829 |
| Popis: |
Current therapy against severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) are based on the use of Remdesivir 1, Molnupiravir 2, and the recently identified Nirmatrelvir 3. Unfortunately, these three drugs showed some limitations regarding potency and possible drug–drug interactions. A series of derivatives coming from a decoration approach of the privileged scaffold s-triazines were synthesized and evaluated against SAR-CoV-2. One derivative emerged as the hit of the series for its micromolar antiviral activity and low cytotoxicity. Mode of action and pharmacokinetic in vitro preliminary studies further confirm the role as candidates for a future optimization campaign of the most active derivative identified with this work. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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