Bioorganic and Medicinal Chemistry p. 4519 - 4527 (2016)
Update date:2022-08-04
Topics:
Shi, Wei-Kang
Deng, Rui-Cheng
Wang, Peng-Fei
Yue, Qin-Qin
Liu, Qi
Ding, Kun-Ling
Yang, Mei-Hui
Zhang, Hong-Yu
Gong, Si-Hua
Deng, Min
Liu, Wen-Run
Feng, Qiu-Ju
Xiao, Zhu-Ping
Zhu, Hai-Liang
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 IC50of 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?1for Kiand Ki′, respectively. The plasma protein binding assays suggested that d24 exhibited moderate binding to human and rabbit plasma proteins.
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