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Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Feb2005, Vol. 15 Issue 4, p883-887. 5p. - Publication Year :
- 2005
-
Abstract
- Abstract: Novel C6-carbamate ketolides with C2-fluorination and C9-oximation have been synthesized. The best compounds in this series displayed MIC values of 0.03–0.12μg/mL against streptococci containing erm and mef resistance determinants and 2–4μg/mL against Haemophilus influenzae. Several compounds also showed measurable activity against erm(B)-containing enterococci with MIC values of 2–8μg/mL. In vivo activity was adversely affected by fluorination, possibly as a result of increased serum protein binding. [Copyright &y& Elsevier]
- Subjects :
- *CARBAMATES
*CARBAMIC acid
*ENTEROCOCCUS
*BLOOD plasma
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 15
- Issue :
- 4
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 16203920
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.12.067