Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors
Copyright © 2021 Elsevier Masson SAS. All rights reserved..
Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:229 |
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| Enthalten in: |
European journal of medicinal chemistry - 229(2022) vom: 05. Feb., Seite 114046 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Stille, Julia K [VerfasserIn] |
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| Links: |
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| Themen: |
3CLpro |
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| Anmerkungen: |
Date Completed 27.01.2022 Date Revised 21.12.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2021.114046 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM335312209 |
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| 520 | |a Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a covalent inhibitors | |
| 650 | 7 | |a Antiviral Agents |2 NLM | |
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| 700 | 1 | |a Tjutrins, Jevgenijs |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Guanyu |e verfasserin |4 aut | |
| 700 | 1 | |a Venegas, Felipe A |e verfasserin |4 aut | |
| 700 | 1 | |a Hennecker, Christopher |e verfasserin |4 aut | |
| 700 | 1 | |a Rueda, Andrés M |e verfasserin |4 aut | |
| 700 | 1 | |a Sharon, Itai |e verfasserin |4 aut | |
| 700 | 1 | |a Blaine, Nicole |e verfasserin |4 aut | |
| 700 | 1 | |a Miron, Caitlin E |e verfasserin |4 aut | |
| 700 | 1 | |a Pinus, Sharon |e verfasserin |4 aut | |
| 700 | 1 | |a Labarre, Anne |e verfasserin |4 aut | |
| 700 | 1 | |a Plescia, Jessica |e verfasserin |4 aut | |
| 700 | 1 | |a Burai Patrascu, Mihai |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Xiaocong |e verfasserin |4 aut | |
| 700 | 1 | |a Wahba, Alexander S |e verfasserin |4 aut | |
| 700 | 1 | |a Vlaho, Danielle |e verfasserin |4 aut | |
| 700 | 1 | |a Huot, Mitchell J |e verfasserin |4 aut | |
| 700 | 1 | |a Schmeing, T Martin |e verfasserin |4 aut | |
| 700 | 1 | |a Mittermaier, Anthony K |e verfasserin |4 aut | |
| 700 | 1 | |a Moitessier, Nicolas |e verfasserin |4 aut | |
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