Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs

Given the crucial role of the main protease (M-pro) in the replication cycle of SARS-CoV-2, this viral cysteine protease constitutes a high-profile drug target. We investigated peptidomimetic azapeptide nitriles as auspicious, irreversibly acting inhibitors of M-pro. Our systematic approach combined...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 67; H. 11; S. 8757 - 8790
Hauptverfasser:	Breidenbach, Julian, Voget, Rabea, Si, Yaoyao, Hingst, Alexandra, Claff, Tobias, Sylvester, Katharina, Wolf, Valentina, Krasniqi, Vesa, Useini, Abibe, Straeter, Norbert, Ogura, Yukino, Kawaguchi, Atsushi, Mueller, Christa E., Guetschow, Michael
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 13.06.2024
Schlagworte:	Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Chemistry, Medicinal Coronavirus 3C Proteases - antagonists & inhibitors Coronavirus 3C Proteases - chemistry Coronavirus 3C Proteases - metabolism COVID-19 Drug Treatment Cysteine Proteinase Inhibitors - chemical synthesis Cysteine Proteinase Inhibitors - chemistry Cysteine Proteinase Inhibitors - pharmacology Drug Discovery Humans Life Sciences & Biomedicine Macrocyclic Compounds - chemical synthesis Macrocyclic Compounds - chemistry Macrocyclic Compounds - pharmacology Nitriles - chemical synthesis Nitriles - chemistry Nitriles - pharmacology Peptides - chemical synthesis Peptides - chemistry Peptides - pharmacology Peptidomimetics - chemical synthesis Peptidomimetics - chemistry Peptidomimetics - pharmacology Pharmacology & Pharmacy Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology SARS-CoV-2 - drug effects Science & Technology Structure-Activity Relationship PLASMA STABILITY COVALENT INHIBITORS ATROPISOMERISM MECHANISM CORONAVIRUS
ISSN:	0022-2623, 1520-4804, 1520-4804
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