Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles

Frederick E Boyer; J V N Vara Prasad; Allison L Choy; Louis Chupak; Michael R Dermyer; Qizhu Ding; Michael D Huband; Wenhua Jiao; Takushi Kaneko; Vladimir Khlebnikov; Ji-Young Kim; Manjinder S Lall; Samarendra N Maiti; Karina Romero; Xiujuan Wu

doi:10.1016/j.bmcl.2007.05.056

Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4694-8. doi: 10.1016/j.bmcl.2007.05.056. Epub 2007 May 24.

Authors

Frederick E Boyer¹, J V N Vara Prasad, Allison L Choy, Louis Chupak, Michael R Dermyer, Qizhu Ding, Michael D Huband, Wenhua Jiao, Takushi Kaneko, Vladimir Khlebnikov, Ji-Young Kim, Manjinder S Lall, Samarendra N Maiti, Karina Romero, Xiujuan Wu

Affiliation

¹ Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. [email protected]

PMID: 17590334
DOI: 10.1016/j.bmcl.2007.05.056

Abstract

A novel series of conformationally-restricted oxazolidinones was synthesized which possess a fused pyrazole ring substituted with various alkyl, aryl and heteroaryl substituents. A number of analogs exhibited potent activity against both gram-positive and fastidious gram-negative organisms.

MeSH terms

Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / pharmacology*
Gram-Negative Bacteria / drug effects*
Gram-Positive Bacteria / drug effects*
Molecular Structure
Oxazolidinones / chemistry*
Oxazolidinones / pharmacology*
Pyrazoles / chemistry
Pyrazoles / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Oxazolidinones
Pyrazoles