Cysteine based novel noncompetitive inhibitors of urease(s)—Distinctive inhibition susceptibility of microbial and plant ureases

Ureases as a target for the treatment of gastric and urinary infections

“…Although some of these compounds are potent urease inhibitors, their safety as well as their in vivo efficiency are yet to be determined 115 116. In addition, several compounds described in the literature display only a moderate inhibitory activity resulting in a low potential for clinical applications 77 117 118. Nevertheless, urease remains as one of the most important targets in the development of drugs for the management of gastric and urinary infections.…”

Synthesis and evaluation of N-analogs of 1,2-diarylethane as Helicobacter pylori urease inhibitors

“…4 In infections with these bacteria, urease is considered to be implicated in urolithiasis (stone formation) and be directly involved in the development of acute pyelonephritis and infection-induced reactive arthritis. [5][6][7] Thus urease inhibition is of very great therapeutic and pharmacological significances. 8 According to recent statistics, at least half of the world population is estimated to be infected by H. pylori, and potent inhibitors of H. pylori urease have increasingly attracted the interests of medicinal chemists.…”

Urease Inhibition

“…Urea and urease are the landmark molecules in the early days of synthetic organic chemistry. Urea was the first organic molecule synthesized in laboratory and urease was being first crystallized out from jack bean (Amtul et al, 2002;Hagar et al, 1925;Mobley et al, 1989;Amtul et al, 2006;Zonia et al, 1995). The significance of the urease enzyme is critically investigated due to its capacity to serve as a virulence factor of infections in the urinary and gastrointestinal tracts, maintaining equilibrium in the nitrogen cycles of nitrogenous wastes in the rumens of domestic livestock, and its importance in environmental transformations of nitrogenous compounds, including urea based fertilizers.…”

“…Urease serves as virulence factor in the pathogens responsible for kidney stones entailed in urolithiasis that contributes toward the acute pyelonephritis with other urinary tract infection which induced arthritis and gastric intestinal infections and ultimately the urease imbalance lead to peptic ulcers (Mobley et al, 1989). Urease controls the nitrogen contents in the physiological systems, while it provides a protection mechanism against predators and phytphathogenic organisms (Amtul et al, 2006;Zonia et al, 1995). The high concentrations of ammonia arising from the biochemical reactions of urease, as well as pH elevation result into important negative implications in medicine and agriculture (Zonia et al, 1995;Collins et al, 1993;Montecucco et al 2001;Zhengping et al).…”