Synthesis and antibacterial activity of 6-O-arylbutynyl ketolides with improved activity against some key erythromycin-resistant pathogens

Robert F Keyes; Justin J Carter; Erika E Englund; Melissa M Daly; Greg G Stone; Angela M Nilius; Zhenkun Ma

doi:10.1021/jm025580k

Synthesis and antibacterial activity of 6-O-arylbutynyl ketolides with improved activity against some key erythromycin-resistant pathogens

J Med Chem. 2003 May 8;46(10):1795-8. doi: 10.1021/jm025580k.

Authors

Robert F Keyes¹, Justin J Carter, Erika E Englund, Melissa M Daly, Greg G Stone, Angela M Nilius, Zhenkun Ma

Affiliation

¹ Infectious Disease Research, Abbott Laboratories, D47P, AP52N, 200 Abbott Park Road, Abbott Park, Illinois 60064-6217, USA. robert.keyes@abbott.com

PMID: 12723941
DOI: 10.1021/jm025580k

Abstract

A series of novel 6-O-substituted homopropargyl ketolides was synthesized and evaluated against various erythromycin-resistant pathogens. Promising in vitro antibacterial activity was demonstrated for compounds bearing this structural motif.

MeSH terms

Alkynes / chemical synthesis*
Alkynes / chemistry
Alkynes / pharmacology
Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology
Drug Resistance, Bacterial
Erythromycin / pharmacology*
Haemophilus influenzae / drug effects
Microbial Sensitivity Tests
Staphylococcus / drug effects
Structure-Activity Relationship

Substances

Alkynes
Anti-Bacterial Agents
Erythromycin