Synthesis and antiviral evaluation of novel peptidomimetics as norovirus protease inhibitors

[Display omitted] A series of tripeptidyl transition state inhibitors with new P1 and warhead moieties were synthesized and evaluated in a GI-1 norovirus replicon system and against GII-4 and GI-1 norovirus proteases. Compound 19, containing a 6-membered ring at the P1 position and a reactive aldehy...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-07, Vol.28 (12), p.2165-2170
Hauptverfasser:	Amblard, Franck, Zhou, Shaoman, Liu, Peng, Yoon, Jack, Cox, Bryan, Muzzarelli, Kendall, Kuiper, Benjamin D., Kovari, Ladislau C., Schinazi, Raymond F.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antiviral Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Cell Line Cell Survival - drug effects Chlorocebus aethiops Dose-Response Relationship, Drug Humans Microbial Sensitivity Tests Molecular Structure Norovirus Norovirus - drug effects Norovirus - enzymology Peptide Peptide Hydrolases - metabolism Peptidomimetics - chemical synthesis Peptidomimetics - chemistry Peptidomimetics - pharmacology Protease inhibitor Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Structure-Activity Relationship Vero Cells Virus Replication - drug effects
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