3-Arylpropionylhydroxamic acid derivatives as Helicobacter pylori urease inhibitors: Synthesis, molecular docking and biological evaluation

Add time:08/14/2019    Source:sciencedirect.com

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 ± 0.05 μM, showing a mixed inhibition with both competitive and uncompetitive aspects. Non-linear fitting of kinetic data gives kinetics parameters of 0.13 and 0.12 μg·mL−1 for Ki and Ki′, respectively. The plasma protein binding assays suggested that d24 exhibited moderate binding to human and rabbit plasma proteins.

We also recommend Trading Suppliers and Manufacturers of salicylic acid, bismuth(3+) salt (cas 15414-77-4). Pls Click Website Link as below: cas 15414-77-4 suppliers

Prev:Simple thermal decomposition of bismuth citrate to Bi/C/α-Bi2O3 with enhanced photocatalytic performance and adsorptive ability
Next:Preparation of acrylic bone cements for vertebroplasty with bismuth salicylate as radiopaque agent)