Strategic Approaches to Overcome Resistance against Gram-Negative Pathogens Using β-Lactamase Inhibitors and β-Lactam Enhancers: Activity of Three Novel Diazabicyclooctanes WCK 5153, Zidebactam (WCK 5107), and WCK 4234

J Med Chem. 2018 May 10;61(9):4067-4086. doi: 10.1021/acs.jmedchem.8b00091. Epub 2018 Apr 20.

Abstract

Limited treatment options exist to combat infections caused by multidrug-resistant (MDR) Gram-negative bacteria possessing broad-spectrum β-lactamases. The design of novel β-lactamase inhibitors is of paramount importance. Here, three novel diazabicyclooctanes (DBOs), WCK 5153, zidebactam (WCK 5107), and WCK 4234 (compounds 1-3, respectively), were synthesized and biochemically characterized against clinically important bacteria. Compound 3 inhibited class A, C, and D β-lactamases with unprecedented k2/ K values against OXA carbapenemases. Compounds 1 and 2 acylated class A and C β-lactamses rapidly but not the tested OXAs. Compounds 1-3 formed highly stable acyl-complexes as demonstrated by mass spectrometry. Crystallography revealed that 1-3 complexed with KPC-2 adopted a "chair conformation" with the sulfate occupying the carboxylate binding region. The cefepime-2 and meropenem-3 combinations were effective in murine peritonitis and neutropenic lung infection models caused by MDR Acinetobacter baumannii. Compounds 1-3 are novel β-lactamase inhibitors that demonstate potent cross-class inhibition, and clinical studies targeting MDR infections are warranted.

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.

MeSH terms

  • Animals
  • Azabicyclo Compounds / chemistry
  • Azabicyclo Compounds / pharmacology*
  • Azabicyclo Compounds / therapeutic use
  • Bridged Bicyclo Compounds / chemistry
  • Bridged Bicyclo Compounds / pharmacology*
  • Bridged Bicyclo Compounds / therapeutic use
  • Cyclooctanes / chemistry
  • Cyclooctanes / pharmacology*
  • Cyclooctanes / therapeutic use
  • Drug Synergism
  • Gram-Negative Bacteria / drug effects*
  • Lung / drug effects
  • Lung / microbiology
  • Mice
  • Octanes / chemistry
  • Octanes / pharmacology*
  • Octanes / therapeutic use
  • Peritonitis / drug therapy
  • Peritonitis / microbiology
  • Piperidines / chemistry
  • Piperidines / pharmacology*
  • Piperidines / therapeutic use
  • beta-Lactam Resistance / drug effects*
  • beta-Lactamase Inhibitors / chemistry
  • beta-Lactamase Inhibitors / pharmacology*
  • beta-Lactamase Inhibitors / therapeutic use
  • beta-Lactamases / metabolism*
  • beta-Lactams / pharmacology*

Substances

  • Azabicyclo Compounds
  • Bridged Bicyclo Compounds
  • Cyclooctanes
  • Octanes
  • Piperidines
  • WCK 4234
  • WCK 5153
  • beta-Lactamase Inhibitors
  • beta-Lactams
  • zidebactam
  • beta-Lactamases