Screening system for urease inhibitors using 13C-NMR.
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.
Chiyoda
T
T
Department of Medicinal Chemistry, Meiji College of Pharmacy, Tokyo, Japan.
Iida
K
K
Takatori
K
K
Kajiwara
M
M
D001667:Binding, Competitive; D001944:Breath Tests / Q000379:methods*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D000431:Ethanol / Q000737:chemistry; D016480:Helicobacter pylori / Q000187:drug effects* / Q000201:enzymology*; D006877:Hydroxamic Acids / Q000494:pharmacology*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy / Q000379:methods*; D009555:Ninhydrin; D013379:Substrate Specificity; D014510:Urease / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D007202:Indicators and Reagents; D000431:Ethanol; C006358:acetohydroxamic acid; D014510:Urease; D009555:Ninhydrin