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

Bioorganic & medicinal chemistry (2015-06-07)
Xu-Dong Wang, Wei Wei, Peng-Fei Wang, Li-Cheng Yi, Wei-Kang Shi, Yong-Xiang Xie, Lang-Zhou Wu, Nian Tang, Liang-Song Zhu, Jia Peng, Chan Liu, Xian-Hui Li, Shi Tang, Zhu-Ping Xiao, Hai-Liang Zhu
ABSTRACT

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 μM) and good anti-H. pylori activity (MIC50=2.6 μg/mL), and it can be used as a good candidate for discovering novel anti-gastric ulcer agent.

MATERIALS
Product Number
Brand
Product Description

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