- Compound, as well as preparation method and application thereof
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The application discloses a compound of which the structure is represented as the following formula, wherein R1 is selected from any one of F, Cl, Br, C1-C5 alkyl group, and a group having the structure as the formula (1), n = 0, 1, 2, 3, 4 or 5; the R2 is selected from any one of a group having the structure as the formula (1), a group having the structure as the formula (2), and a group having the structure as the formula (3). The compound has simple preparation method, can be used as a neuraminidase inhibitor, and has excellent antivirus activity.
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Paragraph 0296-0298; 0302
(2020/03/17)
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- Synthesis, molecular docking and biological evaluation of 3-arylfuran-2(5H)-ones as anti-gastric ulcer agent
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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
- 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
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p. 4860 - 4865
(2015/08/03)
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- Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: Design, synthesis and evaluation as antibacterial agent
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3-Arylfuran-2(5H)-one, a novel antibacterial pharmacophore targeting tyrosyl-tRNA synthetase (TyrRS), was hybridized with the clinically used fluoroquinolones to give a series of novel multi-target antimicrobial agents. Thus, twenty seven 3-arylfuran-2(5H)-one-fluoroquinolone hybrids were synthesized and evaluated for their antimicrobial activities. Some of the hybrids exhibited merits from both parents, displaying a broad spectrum of activity against resistant strains including both Gram-negative and Gram-positive bacteria. The most potent compound (11) in antibacterial assay shows MIC50 of 0.11 μg/mL against Multiple drug resistant Escherichia coli, being about 51-fold more potent than ciprofloxacin. The enzyme assays reveal that 11 is a potent multi-target inhibitor with IC50 of 1.15 ± 0.07 μM against DNA gyrase and 0.12 ± 0.04 μM against TyrRS, respectively. Its excellent inhibitory activities against isolated enzymes and intact cells strongly suggest that 11 deserves to further research as a novel antibiotic.
- Wang, Xu-Dong,Wei, Wei,Wang, Peng-Fei,Tang, Yun-Tao,Deng, Rui-Cheng,Li, Biao,Zhou, Sha-Sha,Zhang, Jing-Wen,Zhang, Lei,Xiao, Zhu-Ping,Ouyang, Hui,Zhu, Hai-Liang
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p. 3620 - 3628
(2014/07/07)
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- A facile synthesis, antibacterial activity of pulvinone and its derivatives
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Pulvinone and several 3-fluoro-4-morpholino substituted pulvinone derivatives were synthesized in five steps from a common precursor, phenyl acetic acid. Most of synthetic morpholine substituted pulvinones showed inhibitory activity against Esherichia col
- Xu, Hai-Wei,Xu, Chao,Fan, Zi-Qi,Zhao, Ling-Jie,Liu, Hong-Min
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p. 737 - 739
(2013/02/25)
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- Synthesis, structure, molecular docking, and structure-activity relationship analysis of enamines: 3-Aryl-4-alkylaminofuran-2(5H)-ones as potential antibacterials
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Thirty-one 3-aryl-4-alkylaminofuran-2(5H)-ones were designed, prepared and tested for their antibacterial activity. Some of them showed significant antibacterial activity against Gram-positive organisms, especially against Staphylococcus aureus ATCC 25923, but all were inactive against Gram-negative organisms. Out of these compounds, 3-(4-bromophenyl)-4-(2-(4-nitrophenyl) hydrazinyl)furan-2(5H)-one (4a11) showed the most potent antibacterial activity against S. aureus ATCC 25923 with MIC50 of 0.42 μg/mL. The enzyme assay revealed that the possible antibacterial mechanism of the synthetic compounds might be due to their inhibitory activity against tyrosyl-tRNA synthetase. Molecular dockings of 4a11 into S. aureus tyrosyl-tRNA synthetase active site were also performed. This inhibitor snugly fitting the active site might well explain its excellent inhibitory activity. Meanwhile, this modeling disclosed that a more suitable optimization strategy might be to modify the benzene ring at 3-position of furanone with hydrophilic groups.
- Xiao, Zhu-Ping,He, Xing-Bing,Peng, Zhi-Yun,Xiong, Tao-Ju,Peng, Juan,Chen, Li-Hua,Zhu, Hai-Liang
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experimental part
p. 1571 - 1579
(2011/04/15)
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- 4-Alkoxy-3-arylfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: Synthesis, molecular docking and antibacterial evaluation
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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
- 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
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experimental part
p. 3884 - 3891
(2011/08/02)
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- Tyrosyl-tRNA synthetase inhibitors as antibacterial agents: Synthesis, molecular docking and structure-activity relationship analysis of 3-aryl-4-arylaminofuran-2(5H)-ones
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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.
- 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
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experimental part
p. 4904 - 4914
(2011/11/29)
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- Synthesis of (E)- and (Z)-Pulvinones
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Two new routes to pulvinones have been developed, one of which involves a novel Wittig reaction.For the first time, members of the E-series, including the parent (E)-pulvinone, are reported and the structural elucidation of the geometric isomers is descri
- Campbell, Alexander C.,Maidment, Maurice S.,Pick, John H.,Stevenson, Donald F. M.
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p. 1567 - 1576
(2007/10/02)
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