Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: Synthesis and optimization studies of benzothiazine-substituted tetramic acids

Benzothiazine-substituted tetramic acids were discovered as highly potent non-nucleoside inhibitors of HCV NS5B polymerase. X-ray crystallography studies confirmed the binding mode of these inhibitors with HCV NS5B polymerase. Rational optimization of time dependent inactivation of CYP 3A4 and clear...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-10, Vol.19 (19), p.5648-5651
Hauptverfasser:	de Vicente, Javier, Hendricks, Robert T., Smith, David B., Fell, Jay B., Fischer, John, Spencer, Stacey R., Stengel, Peter J., Mohr, Peter, Robinson, John E., Blake, James F., Hilgenkamp, Ramona K., Yee, Calvin, Zhao, Junping, Elworthy, Todd R., Tracy, Jahari, Chin, Elbert, Li, Jim, Lui, Al, Wang, Beihan, Oshiro, Connie, Harris, Seth F., Ghate, Manjiri, Leveque, Vincent J.P., Najera, Isabel, Pogam, Sophie Le, Rajyaguru, Sonal, Ao-Ieong, Gloria, Alexandrova, Ludmila, Fitch, Bill, Brandl, Michael, Masjedizadeh, Mohammad, Wu, Shao-yong, Keczer, Steve de, Voronin, Tatyana
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacokinetics Benzothiazine Binding Sites Biological and medical sciences Clearance Crystallography, X-Ray CYP 3A4 HCV Hepacivirus - drug effects Hepatitis C virus Medical sciences NS5B Pharmacology. Drug treatments Pyrrolidinones - chemical synthesis Pyrrolidinones - chemistry Pyrrolidinones - pharmacokinetics Rats Structure-Activity Relationship Tetramic acid Thiazines - chemistry Time dependent inactivation Viral Nonstructural Proteins - antagonists & inhibitors Viral Nonstructural Proteins - metabolism
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