[Substituted 1,5,6,7-tetrahydro-4H-benzimidazol-4-ones as inhibitors of urease].
A comparative kinetic study of the inhibition of urea hydrolysis by 9 substituted 1,5,6,7-tetrahydro-4H-benzimidazol-4-ones (BI I-IX) has been carried out. The inhibition had reversibl competitive character; the inhibition constants K(i), varied from 29 up to 754 microM in dependence of the structure of BI I-IX. Three BI I-III, having the K(i) values from 29 to 82 microM, may be used as the potential therapeutic agents for gastroenterology for treatment of stomach and duodenal ulcers.
Tarun
E I
EI
Zheldakova
T A
TA
Metelitsa
D I
DI
D001562:Benzimidazoles / Q000737:chemistry* / Q000627:therapeutic use; D004381:Duodenal Ulcer / Q000188:drug therapy / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000627:therapeutic use; D006801:Humans; D007700:Kinetics; D010437:Peptic Ulcer / Q000188:drug therapy / Q000201:enzymology; D010940:Plant Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013025:Glycine max / Q000201:enzymology*; D014508:Urea / Q000737:chemistry*; D014510:Urease / Q000037:antagonists & inhibitors* / Q000737:chemistry*
D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D010940:Plant Proteins; D014508:Urea; D014510:Urease