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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 |
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| Authors: | 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 |
| Affiliation: | Pfizer Global Research and Development-La Jolla/Agouron Pharmaceuticals, Inc., San Diego, CA 92121-1111, USA. peter.dragovich@pfizer.com |
| Abstract: | 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). |
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