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

Xenia Beebe; Fan Yang; Mai H Bui; Michael J Mitten; Zhenkun Ma; Angela M Nilius; Stevan W Djuric

doi:10.1016/j.bmcl.2004.03.020

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

Bioorg Med Chem Lett. 2004 May 17;14(10):2417-21. doi: 10.1016/j.bmcl.2004.03.020.

Authors

Xenia Beebe¹, Fan Yang, Mai H Bui, Michael J Mitten, Zhenkun Ma, Angela M Nilius, Stevan W Djuric

Affiliation

¹ Infectious Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA. xenia.b.searle@abbott.com

PMID: 15109624
DOI: 10.1016/j.bmcl.2004.03.020

Abstract

A series of novel 6-O-arylpropargyl-9-oxime-ketolides was synthesized and evaluated against various pathogens. These new compounds show promising in vitro antibacterial potency and in vivo efficacy against macrolide resistant strains.

MeSH terms

Animals
Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / pharmacology
Anti-Bacterial Agents / therapeutic use
Disease Models, Animal
Drug Resistance, Bacterial
Haemophilus influenzae / drug effects
Ketolides / chemical synthesis*
Ketolides / pharmacology*
Ketolides / therapeutic use
Macrolides
Rats
Respiratory Tract Infections / drug therapy
Staphylococcus / drug effects
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Ketolides
Macrolides