Cephalosporin-derived inhibitors of beta-lactamase. Part 4: The C3 substituent

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1663-6. doi: 10.1016/s0960-894x(02)00205-6.


New C3-substituted beta-lactamase inhibitors were prepared and evaluated against representative class A and class C enzymes. It was possible to improve simultaneous inhibitory activity of both classes of serine hydrolase. Other inhibitors showed high selectivity for either the class C cephalosporinases or the class A penicillinases. This represents the first time that cephalosporin-derived inhibitors have demonstrated selectivity for the class A beta-lactamases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cephalosporins / chemistry
  • Cephalosporins / pharmacology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • beta-Lactamase Inhibitors*


  • Cephalosporins
  • Enzyme Inhibitors
  • beta-Lactamase Inhibitors