Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease
Copyright © 2024 Elsevier Masson SAS. All rights reserved..
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and related variants, are responsible for the devastating coronavirus disease 2019 (COVID-19) pandemic. The SARS-CoV-2 main protease (Mpro) plays a central role in the replication of the virus and represents an attractive drug target. Herein, we report the discovery of novel SARS-CoV-2 Mpro covalent inhibitors, including highly effective compound NIP-22c which displays high potency against several key variants and clinically relevant nirmatrelvir Mpro E166V mutants.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:268 |
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| Enthalten in: |
European journal of medicinal chemistry - 268(2024) vom: 15. März, Seite 116263 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Amblard, Franck [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 18.03.2024 Date Revised 12.04.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2024.116263 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM369219287 |
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| 520 | |a Copyright © 2024 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and related variants, are responsible for the devastating coronavirus disease 2019 (COVID-19) pandemic. The SARS-CoV-2 main protease (Mpro) plays a central role in the replication of the virus and represents an attractive drug target. Herein, we report the discovery of novel SARS-CoV-2 Mpro covalent inhibitors, including highly effective compound NIP-22c which displays high potency against several key variants and clinically relevant nirmatrelvir Mpro E166V mutants | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a 3CL(pro) | |
| 650 | 4 | |a Antivirals | |
| 650 | 4 | |a HCoV-OC43 | |
| 650 | 4 | |a Main protease | |
| 650 | 4 | |a Mpro | |
| 650 | 4 | |a NIP-22c | |
| 650 | 4 | |a Peptides | |
| 650 | 4 | |a SARS-CoV-2 | |
| 650 | 7 | |a Peptidomimetics |2 NLM | |
| 650 | 7 | |a Peptide Hydrolases |2 NLM | |
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| 650 | 7 | |a Protease Inhibitors |2 NLM | |
| 650 | 7 | |a Cysteine Endopeptidases |2 NLM | |
| 650 | 7 | |a EC 3.4.22.- |2 NLM | |
| 650 | 7 | |a Antiviral Agents |2 NLM | |
| 700 | 1 | |a LeCher, Julia C |e verfasserin |4 aut | |
| 700 | 1 | |a De, Ramyani |e verfasserin |4 aut | |
| 700 | 1 | |a Zhou, Shaoman |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Peng |e verfasserin |4 aut | |
| 700 | 1 | |a Goh, Shu Ling |e verfasserin |4 aut | |
| 700 | 1 | |a Tao, Sijia |e verfasserin |4 aut | |
| 700 | 1 | |a Patel, Dharmeshkumar |e verfasserin |4 aut | |
| 700 | 1 | |a Downs-Bowen, Jessica |e verfasserin |4 aut | |
| 700 | 1 | |a Zandi, Keivan |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Huanchun |e verfasserin |4 aut | |
| 700 | 1 | |a Chaudhry, Gitika |e verfasserin |4 aut | |
| 700 | 1 | |a McBrayer, Tamara |e verfasserin |4 aut | |
| 700 | 1 | |a Muczynski, Michael |e verfasserin |4 aut | |
| 700 | 1 | |a Al-Homoudi, Abdullah |e verfasserin |4 aut | |
| 700 | 1 | |a Engel, Joseph |e verfasserin |4 aut | |
| 700 | 1 | |a Lan, Shuiyun |e verfasserin |4 aut | |
| 700 | 1 | |a Sarafianos, Stefan G |e verfasserin |4 aut | |
| 700 | 1 | |a Kovari, Ladislau C |e verfasserin |4 aut | |
| 700 | 1 | |a Schinazi, Raymond F |e verfasserin |4 aut | |
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