Enzyme

Cysteine

Proteus

Urease

Bacteria

Escherichia coli

Biology

Microbiology

Gene

Chemistry

Helicobacter pylori

Ebselen

Glutathione peroxidase

Urea

Glutathione

Virulence factor

Genetics

Biochemistry

Virulence

The Chemical Record

Urease, an enzyme that catalyzes the hydrolysis of urea, is a virulence factor of various pathogenic bacteria. In particular, Helicobacter pylori, that colonizes the digestive tract and Proteus spp., that can infect the urinary tract, are related to urease activity. Therefore, urease inhibitors are considered as potential therapeutics against these infections. This review describes current knowledge of the structures, activity, and biological importance of bacterial ureases. Moreover, the structure-based design of several classes of bacterial urease inhibitors is presented and discussed. Phosphinic and phosphonic acids were applied as transition-state analogues, while Michael acceptors and ebselen derivatives were applied as covalent binders of cysteine residue. This review incorporates bacterial urease inhibitors from literature published between 2008 and 2021.

Rational Development of Bacterial Ureases Inhibitors