3-Arylpropionylhydroxamic Acid Derivatives As Helicobacter Pylori Urease Inhibitors: Synthesis, Molecular Docking and Biological Evaluation
Bioorganic & medicinal chemistry(2016)
摘要
Helicobacter pylori urease is involved in several physiologic responses such as stomach and duodenal ulcers, adenocarcinomas and stomach lymphomas. Thus, inhibition of urease is taken for a good chance to treat H. pylori-caused infections, we have therefore focused our efforts on seeking novel urease inhibitors. Here, a series of arylpropionylhydroxamic acids were synthesized and evaluated for urease inhibition. Out of these compounds, 3-(2-benzyloxy-5-chlorophenyl)-3-hydroxypropionylhydroxamic acid (d24) was the most active inhibitor with IC50 of 0.15±0.05μM, showing a mixed inhibition with both competitive and uncompetitive aspects. Non-linear fitting of kinetic data gives kinetics parameters of 0.13 and 0.12μg·mL(-1) for Ki and Ki', respectively. The plasma protein binding assays suggested that d24 exhibited moderate binding to human and rabbit plasma proteins.
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关键词
3-Arylpropionylhydroxamic acid,H. pylori urease inhibitor,Plasma protein binding,Kinetics study,Non-linear fitting
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