Overcoming resistance to β-lactam antibiotics

J Org Chem. 2013 May 3;78(9):4207-13. doi: 10.1021/jo400236f. Epub 2013 Mar 28.


β-Lactam antibiotics are one of the most important antibiotic classes but are plagued by problems of resistance, and the development of new β-lactam antibiotics through side-chain modification of existing β-lactam classes is not keeping pace with resistance development. In this JOCSynopsis, we summarize small molecule strategies to overcome resistance to β-lactam antibiotics. These approaches include the development of β-lactamase inhibitors and compounds that interfere with the ability of the bacteria to sense an antibiotic threat and activate their resistance mechanisms.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Anti-Bacterial Agents* / chemical synthesis
  • Anti-Bacterial Agents* / chemistry
  • Anti-Bacterial Agents* / pharmacology
  • Drug Discovery
  • Molecular Structure
  • Small Molecule Libraries* / chemical synthesis
  • Small Molecule Libraries* / chemistry
  • Small Molecule Libraries* / pharmacology
  • beta-Lactam Resistance / drug effects*
  • beta-Lactamase Inhibitors
  • beta-Lactams* / chemical synthesis
  • beta-Lactams* / chemistry
  • beta-Lactams* / pharmacology


  • Anti-Bacterial Agents
  • Small Molecule Libraries
  • beta-Lactamase Inhibitors
  • beta-Lactams