| Autor: |
Mark Edward Flanagan, Anne E. Hagen, Yue Shen, Dennis Girard, Barbara J. Kamicker, Lou Chupak, Steven M. Finegan, Takushi Kaneko, Usa Reilly, Bryan Li, Timothy J. Strelevitz, R. Scott Obach, Richard A. Buzon, Gregory G. Stone, Karl Granskog, John Schafer, Joanna P. Wolkowski, Thuy-Trinh Nguyen, Mark C. Noe, Donn G. Wishka, Michael J. Falcone, John P. O'Donnell, Thomas J. Dougherty, David A. Whipple, Ivy Medina, Magee Thomas Victor, Joel R. Hardink, Jianmin Sun, Michael D. Huband, Jennifer L. Liras, Sharon L. Ripp, Kathleen A. Farley, Michael J. Knickerbocker, Andrea Marra, A. Tait-Kamradt, Joseph Penzien, Daniel W. Widlicka, Alfin D. N. Vaz |
| Rok vydání: |
2009 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 52(23) |
| ISSN: |
1520-4804 |
| Popis: |
Respiratory tract bacterial strains are becoming increasingly resistant to currently marketed macrolide antibiotics. The current alternative telithromycin (1) from the newer ketolide class of macrolides addresses resistance but is hampered by serious safety concerns, hepatotoxicity in particular. We have discovered a novel series of azetidinyl ketolides that focus on mitigation of hepatotoxicity by minimizing hepatic turnover and time-dependent inactivation of CYP3A isoforms in the liver without compromising the potency and efficacy of 1. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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