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

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.

Graphical abstractA novel series of conformationally-restricted oxazolidinones were synthesized which possess a fused pyrazole ring substituted with various alkyl, aryl and heteroaryl substituentsFigure optionsDownload full-size imageDownload as PowerPoint slide