Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements

Steven D Paget; Christine M Boggs; Barbara D Foleno; Raul M Goldschmidt; Dennis J Hlasta; Michele A Weidner-Wells; Harvey M Werblood; Karen Bush; Mark J Macielag

doi:10.1016/j.bmcl.2006.06.023

Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4537-42. doi: 10.1016/j.bmcl.2006.06.023. Epub 2006 Jun 27.

Authors

Steven D Paget¹, Christine M Boggs, Barbara D Foleno, Raul M Goldschmidt, Dennis J Hlasta, Michele A Weidner-Wells, Harvey M Werblood, Karen Bush, Mark J Macielag

Affiliation

¹ Johnson & Johnson Pharmaceutical Research and Development, LLC, Raritan, NJ 08869, USA.

PMID: 16806921
DOI: 10.1016/j.bmcl.2006.06.023

Abstract

A series of pyrrolopyridine-substituted oxazolidinones containing various C-5 acetamide isosteres was synthesized and the structure-antibacterial activity relationships determined against a representative panel of susceptible and resistant Gram-positive bacteria.

MeSH terms

Acetamides / chemistry*
Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Enterococcus / drug effects
Linezolid
Molecular Structure
Oxazolidinones / chemical synthesis
Oxazolidinones / chemistry*
Oxazolidinones / pharmacology*
Pyridines / chemistry*
Staphylococcus aureus / drug effects
Structure-Activity Relationship

Substances

Acetamides
Anti-Bacterial Agents
Oxazolidinones
Pyridines
acetamide
Linezolid
pyridine