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Inhibition of soybean urease by polycarbonyl compounds

“…It follows from Table 2 that ODH polydisulfide (poly(DSODH)) and cyclic triketones CTKs I-III are the most effective inhibitors of urea hydrolysis. K i values of these compounds are comparable with the values of inhibition constants K i of thiols, many derivatives of hydroxammic acid [8,23], and parameters of thiophosphamides previously measured in our experiments [6]. High inhibition efficacy of poly(disulfidoxalyldihydrazide) is determined by a large number of carbonyl groups in the polymer molecule (~28) and, perhaps, direct interaction of this polymer with urease subunits, the concentration of the enzyme in solution being three to four orders of magnitude lower than concentration of inhibitor.…”

“…pH indicators suggested in [3] and successfully used in our earlier studies [6,9,20,21] is thought to provide the necessary high accuracy of measurement of the initial urea hydrolysis rate at low urease concentration when urease activity is suppressed by inhibitors.…”

“…The main groups of urease inhibitors, specificity and efficiency of urease activity were discussed in our earlier review [6]. It was found that urease was produced by many microorganisms and was associated with such pathologies as duodenal and gastric ulcers as well as a number of human and animal urinary diseases [5,7].…”

“…In earlier studies, we investigated the following urease inhibitors: polydisulfides of urea and thiourea, which compete with the substrate for binding to the urease active sites; amides of thiophosphoric acid, which were analogues of the substituted phosphorodiamidates (these compounds were the most effective urease inhibitors [4][5][6]8]); cyclic β -triketones (CTKs); and fluoride anions. These inhibitors are organic and inorganic ligand chelators of nickel [9].…”

Synthesis, crystal structure, and urease inhibition studies of copper(II) and cobalt(III) complexes with bi(2-fluorobenzylaminoethyl)amine

“…For example, urease serves as a virulence factor in pathogens that are responsible for the development of kidney stones, pyelonephritis, peptic ulcers, and other disease states [4,5]. Therefore, urease inhibition studies have attracted increasing attention [6][7][8][9], and the numerous urease inhibitors have been recently reported [10][11][12][13][14][15][16][17]. For example, thiolic compounds, in which thiolate anions react directly with the metallocenters of ureases [18,19].…”