Literature

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.

DOI： 10.1016/j.bmcl.2004.12.067

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

Bioorganic & Medicinal Chemistry Letters 2005.0

Synthesis and antibacterial activity of 6-O-arylpropargyl-9-oxime-11,12-carbamate ketolides

Bioorganic & Medicinal Chemistry Letters 2004.0

β-Keto-ester chemistry and ketolides. synthesis and antibacterial activity of 2-halogeno, 2-methyl and 2,3 enol-ether ketolides

Bioorganic & Medicinal Chemistry Letters 2000.0

Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics

Bioorganic & Medicinal Chemistry Letters 2004.0

Synthesis and Antibacterial Activity of Ketolides (6-O-Methyl-3-oxoerythromycin Derivatives): A New Class of Antibacterials Highly Potent Against Macrolide-Resistant and -Susceptible Respiratory Pathogens

Journal of Medicinal Chemistry 1998.0

Synthesis and antibacterial evaluation of novel 11-O-carbamoyl clarithromycin ketolides