Urease inhibitors for the treatment of H. pylori

Abstract

Introduction: Helicobacter pylori infects almost half of the World population. Although many infected people are symptom free, the microorganism can still cause a variety of gastrointestinal disorders and gastric adenocarcinoma. It is considered a priority pathogen for the development of new antibiotics by the World Health Organisation (WHO). Many virulence factors of H. pylori have been described. This paper will on H. pylori Urease (HPU).

Area covered: This paper will discuss the (patho)physiology and structure of HPU. In addition, urease inhibitors with known activity against the HPU or inhibitors that show H. pylori growth inhibition will be discussed.

Expert opinion: Increase in selectivity, affinity and potency of HPU inhibitors can be achieved by the design of compounds that interact with distinct regions within the enzyme active site. Especially, covalent interactions seem promising as they clearly effect the dose requirement of the drug candidate.

Keywords: Antibacterials; H. pylori; enzyme inhibitors; growth inhibition; urease enzyme.