Title | 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. | ||
Author | 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 | ||
Journal | Bioorg Med Chem Lett | Publication Year/Month | 2002-Mar |
PMID | 11858991 | PMCID | -N/A- |
Affiliation | 1.Pfizer Global Research and Development-La Jolla/Agouron Pharmaceuticals, Inc., San Diego, CA 92121-1111, USA. peter.dragovich@pfizer.com. |
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 microM).