| Autor: |
Magee TV; Pfizer Global Research & Development, Pfizer, Inc, Groton, Connecticut 06340, USA., Ripp SL, Li B, Buzon RA, Chupak L, Dougherty TJ, Finegan SM, Girard D, Hagen AE, Falcone MJ, Farley KA, Granskog K, Hardink JR, Huband MD, Kamicker BJ, Kaneko T, Knickerbocker MJ, Liras JL, Marra A, Medina I, Nguyen TT, Noe MC, Obach RS, O'Donnell JP, Penzien JB, Reilly UD, Schafer JR, Shen Y, Stone GG, Strelevitz TJ, Sun J, Tait-Kamradt A, Vaz AD, Whipple DA, Widlicka DW, Wishka DG, Wolkowski JP, Flanagan ME |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2009 Dec 10; Vol. 52 (23), pp. 7446-57. |
| DOI: |
10.1021/jm900729s |
| Abstrakt: |
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: |
MEDLINE |
| Externí odkaz: |
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