- 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
(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 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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