Synthesis, molecular docking and biological evaluation of 3-arylfuran-2(5H)-ones as anti-gastric ulcer agent

被引：34

作者：

Wang, Xu-Dong ^{[1
]}

Wei, Wei ^{[1
]}

Wang, Peng-Fei ^{[2
]}

Yi, Li-Cheng ^{[1
,3
]}

Shi, Wei-Kang ^{[1
]}

Xie, Yong-Xiang ^{[1
]}

Wu, Lang-Zhou ^{[1
]}

Tang, Nian ^{[1
]}

Zhu, Liang-Song ^{[1
]}

Peng, Jia ^{[1
]}

Liu, Chan ^{[1
]}

Li, Xian-Hui ^{[1
]}

Tang, Shi ^{[1
]}

Xiao, Zhu-Ping ^{[1
]}

Zhu, Hai-Liang ^{[1
,2
]}

机构：

[1] Jishou Univ, Coll Chem & Chem Engn, Jishou 416000, Peoples R China

[2] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China

[3] Xiangtan Univ, Coll Chem, Xiangtan 411105, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 15期

基金：

中国国家自然科学基金;

关键词：

3-Arylfuran-2(5H)-one; Anti-H; pylori; Antioxidant; TyrRS; Gastric ulcer treatment; HELICOBACTER-PYLORI UREASE; RNA SYNTHETASE SYNTHESIS; IN-VITRO; ANTIBACTERIAL EVALUATION; ANTIOXIDANT PROPERTIES; HUMAN NEUTROPHILS; PULVINIC ACIDS; INHIBITORS; INFECTION; DERIVATIVES;

D O I：

10.1016/j.bmc.2015.05.026

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

3-Arylfuran-2(5H)-one derivatives show good antibacterial activity and were determined as tyrosyl-tRNA synthetase (TyrRS) inhibitors. In a systematic medicinal chemistry exploration, we demonstrated chemical opportunities to treat infections caused by Helicobacter pylori. Twenty 3-arylfuran-2(5H)-ones were synthesized and evaluated for anti-H. pylori, antioxidant and anti-urease activities which are closely interconnected with H. pylori infection. The results displayed that some of the compounds show excellent antioxidant activity, and good anti-H. pylori and urease inhibitory activities. Out of these compounds, 3( 3-methylphenyl) furan-2(5H)-one (b9) showed the most potent antioxidant activity (IC50 = 8.2 mu M) and good anti-H. pylori activity (MIC50 = 2.6 mu g/mL), and it can be used as a good candidate for discovering novel anti-gastric ulcer agent. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4860 / 4865

页数：6

共 39 条

[1]

Arend Andres, 2005, Medicina (Kaunas), V41, P343

[2]

Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones [J].