Structure-based design of β-lactamase inhibitors. 1. Synthesis and evaluation of bridged monobactams

Article abstract of DOI:10.1021/jm980023c

Bridged monobactams are novel, potent, mechanism-based inhibitors of class C β-lactamases, designed using X-ray crystal structures of the enzymes. They stabilize the acyl-enzyme intermediate by blocking access of water to the enzyme-inhibitor ester bond.