Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes |
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| Authors: | Xu Xiaodong Henninger Todd Abbanat Darren Bush Karen Foleno Barbara Hilliard Jamese Macielag Mark |
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| Institution: | Antimicrobial Agents Research Team, Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. xxu@prdus.jnj.com |
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| Abstract: | Novel C6-carbamate ketolides with C2-fluorination and C9-oximation have been synthesized. The best compounds in this series displayed MIC values of 0.03-0.12 microg/mL against streptococci containing erm and mef resistance determinants and 2-4 microg/mL against Haemophilus influenzae. Several compounds also showed measurable activity against erm(B)-containing enterococci with MIC values of 2-8 microg/mL. In vivo activity was adversely affected by fluorination, possibly as a result of increased serum protein binding. |
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