Synthesis, molecular docking and biological evaluation of 3-arylfuran-2(5H)-ones as anti-gastric ulcer agent. Issue 15 (1st August 2015)

• Record Type: Journal Article
• Authors: Wang, Xu-Dong; Wei, Wei; Wang, Peng-Fei; Yi, Li-Cheng; Shi, Wei-Kang; Xie, Yong-Xiang; Wu, Lang-Zhou; Tang, Nian; Zhu, Liang-Song; Peng, Jia; Liu, Chan; Li, Xian-Hui; Tang, Shi; Xiao, Zhu-Ping; Zhu, Hai-Liang
• Is Part Of: Bioorganic & medicinal chemistry. Volume 23:Issue 15(2015)
• Page Start: 4860
• Page End: 4865
• Publication Date: 2015-08-01
• Subjects: 3-Arylfuran-2(5H)-one -- Anti-H. pylori -- Antioxidant -- TyrRS -- Gastric ulcer treatment; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2015.05.026
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: 3-Arylfuran-2(5 H )-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(5 H )-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(5 H )-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.