1. Synthesis and antibacterial activity of C6-carbazate ketolides.
- Author
-
Tennakoon MA, Henninger TC, Abbanat D, Foleno BD, Hilliard JJ, Bush K, and Macielag MJ
- Subjects
- Microbial Sensitivity Tests, Structure-Activity Relationship, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents pharmacology, Hydrazines, Ketolides chemical synthesis, Ketolides pharmacology, Staphylococcus drug effects
- Abstract
A novel series of ketolides containing heteroaryl groups that are linked to the erythronolide ring via a C6-carbazate functionality has been successfully synthesized. Careful modulation of the heteroaryl groups, the length and degree of saturation of the C6-carbazate linker, and the substituents present on each of the carbazate nitrogens led to compounds with potent activity against key bacterial respiratory pathogens. The best analogs of this series had in vitro and in vivo (sc dosing) profiles that were comparable to telithromycin.
- Published
- 2006
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