Urease inhibitors as potential drugs for gastric and urinary tract infections: a patent review

Expert Opin Ther Pat. 2011 Jun;21(6):945-57. doi: 10.1517/13543776.2011.574615. Epub 2011 Apr 4.


Introduction: Urease is the enzyme that catalyzes the hydrolysis of urea, which is involved in serious infections caused by Helicobacter pylori in the gastric tract, as well as Proteus and related species in the urinary tract. The necessity to treat such infections has stimulated intensive studies on various groups of urease inhibitors.

Areas covered: Patent literature on urease inhibitors with possible applications in medicine is reviewed in this paper. Hydroxamic acids, phosphoramidates, urea derivatives, quinones and heterocyclic compounds constitute the major classes of structures with such activity.

Expert opinion: Until now, only one compound, acetohydroxamic acid, has been clinically used for the treatment of urinary tract infections by urease inhibition. Unfortunately, it exhibits severe side effects. Thus, it seems that the full potential of urease inhibition has not yet been fully explored. Several Japanese patents related to the use of herbal extracts as sources of polyphenolic urease inhibitors have been considered as complementary or alternative therapy; however, their accessibility is quite possibly due to reduced restrictions for the introduction of natural products to the market.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amides / therapeutic use
  • Enzyme Inhibitors / therapeutic use*
  • Helicobacter Infections / drug therapy*
  • Helicobacter pylori*
  • Humans
  • Hydroxamic Acids / therapeutic use
  • Patents as Topic*
  • Phosphoric Acids / therapeutic use
  • Urea / analogs & derivatives
  • Urease / antagonists & inhibitors*
  • Urinary Tract Infections / drug therapy*


  • Amides
  • Enzyme Inhibitors
  • Hydroxamic Acids
  • Phosphoric Acids
  • Urea
  • phosphoramidic acid
  • Urease