Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. Part 7: Structure–Activity Studies of Bicyclic 2-Pyridone-Containing Peptidomimetics

The structure-based design, chemical synthesis, and biological evaluation of bicyclic 2-pyridone-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors are described. An optimized compound is shown to exhibit antiviral activity when tested against a variety of HRV serotypes (EC 50's ran...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-03, Vol.12 (5), p.733-738
Hauptverfasser:	Dragovich, Peter S., Prins, Thomas J., Zhou, Ru, Johnson, Theodore O., Brown, Edward L., Maldonado, Fausto C., Fuhrman, Shella A., Zalman, Leora S., Patick, Amy K., Matthews, David A., Hou, Xinjun, Meador, James W., Ferre, Rose Ann, Worland, Stephen T.
Format:	Artikel
Sprache:	eng
Schlagworte:	3C Viral Proteases Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Antiviral Agents - chemical synthesis Antiviral Agents - pharmacology Biological and medical sciences Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis Bridged Bicyclo Compounds, Heterocyclic - chemistry Bridged Bicyclo Compounds, Heterocyclic - pharmacology Cell Line Cysteine Endopeptidases Cysteine Proteinase Inhibitors - chemical synthesis Cysteine Proteinase Inhibitors - pharmacology Drug Design Humans Medical sciences Molecular Mimicry Pharmacology. Drug treatments Pyridones - chemical synthesis Pyridones - chemistry Pyridones - pharmacology Rhinovirus - drug effects Rhinovirus - enzymology Serotyping Structure-Activity Relationship Viral Proteins - antagonists & inhibitors
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Zusammenfassung:	The structure-based design, chemical synthesis, and biological evaluation of bicyclic 2-pyridone-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors are described. An optimized compound is shown to exhibit antiviral activity when tested against a variety of HRV serotypes (EC 50's ranging from 0.037 to 0.162 μM). Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00008-2