Title of article
Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes
Author/Authors
Xiaodong Xu، نويسنده , , Todd Henninger، نويسنده , , Darren Abbanat، نويسنده , , Karen Bush and Osnat Herzberg، نويسنده , , Barbara Foleno، نويسنده , , Jamese Hilliard، نويسنده , , Mark Macielag، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
883
To page
887
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 μg/mL against streptococci containing erm and mef resistance determinants and 2–4 μg/mL against Haemophilus influenzae. Several compounds also showed measurable activity against erm(B)-containing enterococci with MIC values of 2–8 μg/mL. In vivo activity was adversely affected by fluorination, possibly as a result of increased serum protein binding.
Keywords
Ketolide , Carbamate , Fluoro ketolide , resistant bacteria , oxime
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795303
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