Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria

Bioorg Med Chem Lett. 2019 Dec 1;29(23):126747. doi: 10.1016/j.bmcl.2019.126747. Epub 2019 Oct 21.

Abstract

A series of novel biaryloxazolidinone derivatives containing amide and acrylamide structure were designed, synthesized and evaluated for their antibacterial activity. Most compounds generally exhibited potent antibacterial activity with MIC values of 1 μg/mL against S. aureus, MRSA, MSSA, LREF and VRE pathogens, using linezolid and radezolid as positive controls. Compound 17 exhibited good antibacterial activity with MIC values of 0.5 μg/mL against S. aureus, MRSA, MSSA and VRE and 0.25 μg/mL against LREF. The results indicated that compound 17 might serve as a potential hit-compound for further investigation.

Keywords: Antibacterial activity; Biaryloxazolidinone; Gram-positive bacteria.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylamide / chemical synthesis*
  • Amides / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use*
  • Gram-Positive Bacteria / drug effects*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Amides
  • Anti-Bacterial Agents
  • Acrylamide