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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Xu X,Henninger T,Abbanat D,Bush K,Foleno B,Hilliard J,Macielag M

doi

10.1016/j.bmcl.2004.12.067

subject

Has Abstract

pub_date

2005-02-15 00:00:00

pages

883-7

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01529-X

journal_volume

15

pub_type

杂志文章

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