Details

Autor(en) / Beteiligte

• Magee, Thomas V
• Ripp, Sharon L
• Li, Bryan
• Buzon, Richard A
• Chupak, Lou
• Dougherty, Thomas J
• Finegan, Steven M
• Girard, Dennis
• Hagen, Anne E
• Falcone, Michael J
• Farley, Kathleen A
• Granskog, Karl
• Hardink, Joel R
• Huband, Michael D
• Kamicker, Barbara J
• Kaneko, Takushi
• Knickerbocker, Michael J
• Liras, Jennifer L
• Marra, Andrea
• Medina, Ivy
• Nguyen, Thuy-Trinh
• Noe, Mark C
• Obach, R. Scott
• O’Donnell, John P
• Penzien, Joseph B
• Reilly, Usa Datta
• Schafer, John R
• Shen, Yue
• Stone, Gregory G
• Strelevitz, Timothy J
• Sun, Jianmin
• Tait-Kamradt, Amelia
• Vaz, Alfin D. N
• Whipple, David A
• Widlicka, Daniel W
• Wishka, Donn G
• Wolkowski, Joanna P
• Flanagan, Mark E

Titel

Discovery of Azetidinyl Ketolides for the Treatment of Susceptible and Multidrug Resistant Community-Acquired Respiratory Tract Infections

Ist Teil von

• Journal of medicinal chemistry, 2009-12, Vol.52 (23), p.7446-7457

Ort / Verlag

Columbus, OH: American Chemical Society

Erscheinungsjahr

2009

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.