Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 8. Pharmacological optimization of orally …

…, EL Brown, FC Maldonado, T Tuntland…

文献索引：Dragovich, Peter S.; Prins, Thomas J.; Zhou, Ru; Johnson, Theodore O.; Hua, Ye; Luu, Hiep T.; Sakata, Sylvie K.; Brown, Edward L.; Maldonado, Fausto C.; Tuntland, Tove; Lee, Caroline A.; Fuhrman, Shella A.; Zalman, Leora S.; Patick, Amy K.; Matthews, David A.; Wu, Ellen Y.; Guo, Ming; Borer, Bennett C.; Nayyar, Naresh K.; Moran, Terence; Chen, Lijian; Rejto, Paul A.; Rose, Peter W.; Guzman, Mark C.; Dovalsantos, Elena Z.; Lee, Steven; McGee, Kevin; Mohajeri, Michael; Liese, Andreas; Tao, Junhua; Kosa, Maha B.; Liu, Bo; Batugo, Minerva R.; Gleeson, Jean-Paul R.; Wu, Zhen Ping; Liu, Jia; Meador III, James W.; Ferre, Rose Ann Journal of Medicinal Chemistry, 2003 , vol. 46, # 21 p. 4572 - 4585

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被引用次数: 81

摘要

The optimization of the pharmacokinetic performance of various 2-pyridone-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors following oral administration to either beagle dogs or CM-monkeys is described. The molecules described in this work are composed of a 2-pyridone-containing peptidomimetic binding determinant and an α, β- unsaturated ester Michael acceptor moiety which forms an irreversible covalent adduct ...