100074-37-1Relevant articles and documents
Compound, as well as preparation method and application thereof
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Paragraph 0296-0298; 0302, (2020/03/17)
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.
Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: Design, synthesis and evaluation as antibacterial agent
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
, p. 3620 - 3628 (2014/07/07)
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.
Synthesis, structure, molecular docking, and structure-activity relationship analysis of enamines: 3-Aryl-4-alkylaminofuran-2(5H)-ones as potential antibacterials
Xiao, Zhu-Ping,He, Xing-Bing,Peng, Zhi-Yun,Xiong, Tao-Ju,Peng, Juan,Chen, Li-Hua,Zhu, Hai-Liang
experimental part, p. 1571 - 1579 (2011/04/15)
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.