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Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes

Authors :
Xu, Xiaodong
Henninger, Todd
Abbanat, Darren
Bush, Karen
Foleno, Barbara
Hilliard, Jamese
Macielag, Mark
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]

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