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β-Lactam Antibiotics


  1. Sebastian A. Testero,
  2. Jed F. Fisher,
  3. Shahriar Mobashery

Published Online: 15 SEP 2010

DOI: 10.1002/0471266949.bmc226

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Testero, S. A., Fisher, J. F. and Mobashery, S. 2010. β-Lactam Antibiotics. Burger's Medicinal Chemistry and Drug Discovery. 257–402.

Author Information

  1. Department of Chemistry and Biochemistry, The University of Notre Dame, Notre Dame, IN

Publication History

  1. Published Online: 15 SEP 2010


The β-lactam classes of antibacterials are preeminent in the treatment of bacterial infection due to their unparalleled clinical efficacy and clinical safety. Following the discovery of the penicillins, successive β-lactam drug discovery has added the cephalosporin, penem cephamycin, clavulanate, monobactam, nocardicin, and carbapenem subclasses. The driving force behind much of this era of discovery is the staggering ability of pathogenic bacteria to adapt previous generations of the β-lactam by the acquisition and expression of resistance mechanisms. Although many factors contribute to β-lactam resistance, alterations to the molecular targets of the β-lactams (the penicillin binding proteins) and the use of enzymes (the β-lactamases) capable of the hydrolytic deactivation of the β-lactams are paramount. This review traces the historical development of β-lactam drug discovery, with emphasis on the most recent progress in the medicinal chemistry, biochemistry, and microbiology of the β-lactams leading to the discovery of new generation β-lactam antibacterials effective against the Gram-negative and -positive bacterial pathogens of current medical concern.


  • β-lactam;
  • β-lactamase;
  • penicillin;
  • cephalosporin;
  • monobactam