Privileged Scaffold Decoration for the Identification of the First Trisubstituted Triazine with Anti-SARS-CoV-2 Activity
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:27 |
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| Enthalten in: |
Molecules (Basel, Switzerland) - 27(2022), 24 vom: 12. Dez. |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Cesarini, Silvia [VerfasserIn] |
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| Links: |
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| Themen: |
Antiviral Agents |
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| Anmerkungen: |
Date Completed 26.12.2022 Date Revised 26.12.2022 published: Electronic Citation Status MEDLINE |
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| doi: |
10.3390/molecules27248829 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM350694842 |
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| 245 | 1 | 0 | |a Privileged Scaffold Decoration for the Identification of the First Trisubstituted Triazine with Anti-SARS-CoV-2 Activity |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Vicenti, Ilaria |e verfasserin |4 aut | |
| 700 | 1 | |a Poggialini, Federica |e verfasserin |4 aut | |
| 700 | 1 | |a Secchi, Massimiliano |e verfasserin |4 aut | |
| 700 | 1 | |a Giammarino, Federica |e verfasserin |4 aut | |
| 700 | 1 | |a Varasi, Ilenia |e verfasserin |4 aut | |
| 700 | 1 | |a Lodola, Camilla |e verfasserin |4 aut | |
| 700 | 1 | |a Zazzi, Maurizio |e verfasserin |4 aut | |
| 700 | 1 | |a Dreassi, Elena |e verfasserin |4 aut | |
| 700 | 1 | |a Maga, Giovanni |e verfasserin |4 aut | |
| 700 | 1 | |a Botta, Lorenzo |e verfasserin |4 aut | |
| 700 | 1 | |a Saladino, Raffaele |e verfasserin |4 aut | |
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