Substituted 1,5,6,7-tetrahydro-4h-benzimidazol-4-ones as inhibitors of urease

   
Tarun E.I.1 , Zheldakova T.A.1, Metelitza D.I.1

1. Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus
Section: Experimental/Clinical Study
UDK: 577.152.3      PubMed Id: 19105401
Year: 2008  Volume: 54  Issue: 5  Pages: 588-596
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 reversible competitive character; the inhibition constants Ki, varied from 29 up to 754 μM in dependence of the structure of BI I-IX. Three BI I-III, having the Ki values from 29 to 82 μM, may be used as the potential therapeutic agents for gastroenterology for treatment of stomach and duodenal ulcers.
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Tarun E.I., Zheldakova T.A., Metelitza D.I. (2008) Biomeditsinskaya khimiya, 54(5), 588-596.
This paper is also available as the English translation:10.1134/S1990750809010107
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