115883-14-2Relevant academic research and scientific papers
Synthesis, molecular docking and biological evaluation of 3-arylfuran-2(5H)-ones as anti-gastric ulcer agent
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
, p. 4860 - 4865 (2015)
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 Hel
4-Alkoxy-3-arylfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: Synthesis, molecular docking and antibacterial evaluation
Xiao, Zhu-Ping,Ouyang, Hui,Wang, Xu-Dong,Lv, Peng-Cheng,Huang, Ze-Jun,Yu, She-Rong,Yi, Tian-Fang,Yang, Ye-Ling,Zhu, Hai-Liang
experimental part, p. 3884 - 3891 (2011/08/02)
A series of novel 4-alkoxy-3-arylfuran-2(5H)-ones as tyrosyl-tRNA synthetase inhibitors were synthesized. Of these compounds, 3-(4-hydroxyphenyl)- 4-(2-morpholinoethoxy)furan-2(5H)-one (27) was the most potent. The binding model and structure-activity rel
Tyrosyl-tRNA synthetase inhibitors as antibacterial agents: Synthesis, molecular docking and structure-activity relationship analysis of 3-aryl-4-arylaminofuran-2(5H)-ones
Xiao, Zhu-Ping,Ma, Tao-Wu,Liao, Mei-Lin,Feng, Yu-Ting,Peng, Xiao-Chun,Li, Jia-Liang,Li, Zhi-Ping,Wu, Ying,Luo, Qun,Deng, Yang,Liang, Xiao,Zhu, Hai-Liang
experimental part, p. 4904 - 4914 (2011/11/29)
Thirty-five 3-aryl-4-arylaminofuran-2(5H)-one derivatives were designed, prepared and tested for their inhibitory activity against tyrosyl-tRNA synthetase. Out of these compounds, 3-(3-bromophenyl)-4-(3,5- dichlorophenylamino)furan-2(5H)-one (35) was the most active with IC 50 of 0.09 ± 0.02 μM. The structure-activity relationship revealed that introduction of chlorine atoms at both meta positions of aniline moiety significantly increased the enzyme inhibitory activity. The results of antibacterial assay revealed that the tested compounds showed good activity against Gram-positive bacteria, with 35 being the most potent with MIC 50 of 0.06 μg/mL against Staphylococcus aureus ATCC 25923. Molecular docking of 35 into S. aureus tyrosyl-tRNA synthetase active site was also performed. The inhibitor snugly fitting the active site may well explain its excellent inhibitory activity.
