Screening system for urease inhibitors using 13C-NMR

Chem Pharm Bull (Tokyo). 1998 Apr;46(4):718-20. doi: 10.1248/cpb.46.718.

Abstract

Urease inhibitors are candidate drugs to treat infection with the human pathogen, Helicobacter pylori, which produces a potent urease [urea amidohydrolase; EC 3.5.1.5]. We developed a screening system based on 13C-NMR measurement of the time course of decrease in the signal of 13C-urea in the presence of urease. The effect on urease activity of known inhibitors, hydroxamic acids, L-ascorbic acid, 2,2'-dipyridyl disulfide and ninhydrin, was speedily and conveniently measured by this method.

MeSH terms

  • Binding, Competitive
  • Breath Tests / methods*
  • Enzyme Inhibitors / pharmacology*
  • Ethanol / chemistry
  • Helicobacter pylori / drug effects*
  • Helicobacter pylori / enzymology*
  • Hydroxamic Acids / pharmacology*
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy / methods*
  • Ninhydrin
  • Substrate Specificity
  • Urease / antagonists & inhibitors*

Substances

  • Enzyme Inhibitors
  • Hydroxamic Acids
  • Indicators and Reagents
  • Ethanol
  • acetohydroxamic acid
  • Urease
  • Ninhydrin