- Synthesis and bio-evaluation of natural butenolides-acrylate conjugates
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A series of novel 3-aryl-4-hydroxy-2(5H) furanone-acrylate hybrids were designed and synthesized based on the natural butenolides and acrylates scaffolds. The structures of the prepared compounds were characterized by 1H-NMR, 13C-NMR and electrospray ionization mass spectrometry (ESI-MS), and the bioactivity of the target compounds against twelve phytopathogenic fungi was investigated. The preliminary in vitro antifungal activity screening showed that most of the target compounds had moderate inhibition on various pathogenic fungi at the concentration of 100 mg·L?1, and presented broad-spectrum antifungal activities. Further studies also indicated that compounds 7e and 7k still showed some inhibitory activity against Pestallozzia theae, Sclerotinia sclerotiorum and Gibberella zeae on rape plants at lower concentrations, which could be optimized as a secondary lead for further research.
- Bao, Longzhu,Wang, Shuangshuang,Song, Di,Wang, Jingjing,Cao, Xiufang,Ke, Shaoyong
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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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- 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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