Synthesis, molecular docking and kinetic properties of β-hydroxy-β-phenylpropionyl-hydroxamic acids as Helicobacter pylori urease inhibitors

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期刊论文

作者：

Xiao, Zhu-Ping*;Peng, Zhi-Yun;Dong, Jing-Jun;Deng, Rui-Cheng;Wang, Xu-Dong;...

通讯作者：

Xiao, Zhu-Ping

作者机构：

[Yang, Pan; Wang, Xu-Dong; Zhu, Man; He, Juan; Zhu, Hai-Liang; Xiao, Zhu-Ping; Peng, Wan-Xi; Peng, Zhi-Yun; Ouyang, Hui; Wang, Yuan-Feng; Peng, Xiao-Chun; Deng, Rui-Cheng] Jishou Univ, Coll Chem & Chem Engn, Key Lab Hunan Forest Prod & Chem Ind Engn, Jishou 416000, Peoples R China.

[Zhu, Hai-Liang; Dong, Jing-Jun] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China.

[Peng, Wan-Xi] Cent South Univ Forestry & Technol, Sch Mat Sci & Engn, Changsha 410004, Hunan, Peoples R China.

通讯机构：

[Xiao, Zhu-Ping] J

Jishou Univ, Coll Chem & Chem Engn, Key Lab Hunan Forest Prod & Chem Ind Engn, Jishou 416000, Peoples R China.

语种：

英文

关键词：

A mixture of competitive and uncompetitive mechanism;Helicobacter pylori urease;Hydroxamic acid;Inhibitor

期刊：

European Journal of Medicinal Chemistry

ISSN：

0223-5234

年：

2013

卷：

页码：

212-221

DOI：

10.1016/j.ejmech.2013.07.047

基金类别：

National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81273382, 31100421]; Hunan Provincial Natural Science Foundation of ChinaNatural Science Foundation of Hunan Province [11JJ3113, 13JJ2030]; aid program for Science and Technology Innovative Research Team (Chemicals of Forestry Resources and Development of Forest Products) in Higher Educational Institutions of Hunan Province

机构署名：

本校为其他机构

院系归属：

材料科学与工程学院

摘要：

Inhibition of urease results in Helicobacter pylori growth arrest in the stomach, promoting urease as promising targets for gastrointestinal ulcer therapy. Twenty hybrid derivatives of flavonoid scaffold and hydroxamic acid, β-hydroxy-β-phenylpropionylhydroxamic acids, were therefore synthesized and evaluated against H. pylori urease. Biological evaluation of these compounds showed improved urease inhibition exhibiting micromolar to mid-nanomolar IC50 values. Most importantly, 3-(3-chlorophenyl)-3- hydroxypropionyl-hydroxamic acid (6g) exhibi...

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Synthesis, molecular docking and kinetic properties of β-hydroxy-β-phenylpropionyl-hydroxamic acids as Helicobacter pylori urease inhibitors

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