185033-52-7Relevant academic research and scientific papers
Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents
Miao, Yuhang,Sun, Jie,Wang, Xiaojing,Yang, Jie,Yun, Yinling
, (2020/01/03)
Alzheimer's disease (AD) is a progressive neurological degenerative disease that has complex pathogenesis. A variety of studies in humans indicate that several enzymes inhibitors can be useful in the treatment of AD, including acetylcholinesterase (AchE), butyrylcholinesterase (BuChE) and monoamine oxidase (MAO). Various substituted 4-arylcoumarin derivatives were synthesised, and their activity in vitro were investigated, including AChE/BuChE inhibitory activity, MAO inhibitory activity, and antioxidant activity. Most of the compounds were found to exhibit high inhibitory activity, and individual compounds have extremely excellent activities. Therefore 4-arylcoumarins provides an idea for drugs design for the development of therapeutic or preventive agents for AD.
Synthesis and biological evaluation of novel neoflavonoid derivatives as potential antidiabetic agents
Wang, Bing,Li, Na,Liu, Teng,Sun, Jie,Wang, Xiaojing
, p. 34448 - 34460 (2017/07/22)
Various substituted neoflavonoid derivatives were synthesized using sulfated montmorillonite K-10 as a catalyst. This method is environmental friendly, sustainable and economical, convenient in isolation and purification processes, with little byproducts, using earth-abundant catalysts and has relatively high yield. Those neoflavonoid derivatives were screened for antioxidant, a-glucosidase inhibitory, aldose reductase 2 (ALR2) inhibitory and advanced glycation end-product formation inhibitory effects. Most compounds exhibited significant antioxidant and advanced glycation end-product (AGE) formation inhibitory activities. It was interesting to note that out of thirty compounds, 8k and 8l were found to have greater ALR2 inhibitory activity than the standard drug quercetin. The pharmacological studies suggested neoflavonoid with adjacent 7,8-dihydroxy groups were more effective in inhibiting ALR2. Antidiabetic activity studies had shown that compounds 8l and 8m were equipotent to the standard drug glibenclamide in vivo. In summary, the target compound 8l provided a potential drug design concept for the development of therapeutic or prophylactic agents of diabetes and diabetes complications.
Preparation method of neoflavonoids
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, (2017/04/26)
The invention relates to the field of chemical synthesis, in particular to a preparation method of neoflavonoids. The preparation method is characterized by comprising the following steps of using substituted benzaldehyde as an initial raw material to be reacted with malonic acid to generate a substituted phenylacrylic acid compound; performing an addition reaction, an elimination reaction and the like on the substituted phenylacrylic acid compound, or performing acetylation so as to protect a phenolic hydroxyl group, then performing a bromination reaction and the elimination reaction so as to synthesize the substituted phenylpropiolic acid compound ; and using montmorillonite K-10 after being acidulated by sulfuric acid as a catalyst, enabling the substituted phenylpropiolic acid compound and a phenolic compound to perform a heating reaction so as to generate the neoflavonoids. Compared with the prior art, the preparation method of the neoflavonoids, disclosed by the invention, has the characteristics that raw materials are cheap, and easy to obtain, the operation is simple, the catalyst can be recovered for use, and the method is environmentally-friendly, the post-treatment is simple, and the production cost is low, and the method has a high popularization and application value.
Synthesis of selected 3- and 4-arylcoumarin derivatives and evaluation as potent antioxidants
Danis, Ozkan,Demir, Serap,Gunduz, Cihan,Alparslan, Mustafa Muhlis,Altun, Selcuk,Yuce-Dursun, Basak
, p. 6061 - 6077 (2016/06/01)
A series of hydroxyl-, methoxy-, and acetoxy-substituted 3- and 4-arylcoumarins were synthesized. All title compounds were screened for their antioxidant capacity, ability to scavenge the 1,1-diphenyl-1-picrylhydrazyl (DPPH) radical, and ability to chelat
Synthesis and anticancer activity of 7,8-dihydroxy-4-arylcoumarins
Wu, Jianrui,Peng, Ting,Chen, Fang,Leng, Yixin,Tong, Linjiang,Li, Mengyuan,Qu, Rong,Xie, Hua,Ding, Jian,Duan, Wenhu
, p. 366 - 373 (2015/06/22)
A series of 7,8-dihydroxy-4-arylcoumarins, the derivatives related to DW532 that was an anti-tumor agent targeting both kinase and tubulin, was prepared by Suzuki coupling reaction. Among them, compounds 6a, 6b, and 6c were found to exhibit anti-prolifera
Antioxidant and antitumor activities of 4-arylcoumarins and 4-aryl-3,4-dihydrocoumarins
Zhang, Keyun,Ding, Weixian,Sun, Jie,Zhang, Bin,Lu, Fujiao,Lai, Ren,Zou, Yong,Yedid, Gabriel
supporting information, p. 203 - 210 (2015/02/19)
Five 4-arylcoumarins (1c-g) and twelve 3,4-dihydro-4-arylcoumarins (2a-l) were synthesized and tested for antioxidant activity, antitumor activity, toxicity and structure-activity relationships analysis. 4-Arylcoumarins and 3,4-dihydro-4-arylcoumarins tha
Synthesis and NMR of 4-Aryl-3,4-dihydrocoumarins and 4-arylcoumarins
Sun, Jie,Wang, Yanfeng
, p. 7753 - 7758 (2015/02/02)
This paper described the synthesis and 1H and 13C NMR chemical shifts of a series of 4-aryl-3,4-dihydrocoumarin and 4-arylcoumarin derivatives based on a combination of 1H and 13C NMR, HSQC and HMBC experiments.
Synthesis and antimicrobial activities of 4-aryl-3,4-dihydrocoumarins and 4-arylcoumarins
Sun, Jie,Ding, Wei-Xian,Hong, Xiao-Ping,Zhang, Ke-Yun,Zou, Yong
, p. 16 - 22 (2012/07/28)
A new series of 4-aryl-3,4-dihydrocoumarins and 4-arylcoumarins were synthesized by the reaction of substituted cinnamic acids and 3-arylpropiolic acid with the corresponding phenols. These compounds were evaluated for antibacterial activity in vitro. The
Efficient synthesis and biological evaluation of 4-arylcoumarin derivatives
Sun, Jie,Ding, Wei Xian,Zhang, Ke Yun,Zou, Yong
scheme or table, p. 667 - 670 (2012/01/13)
Two bioactive natural 4-arylcoumarins, 5,7,4′-trimethoxy-4- phenylcoumarin (1a), 5,7-dimethoxy-4-phenylcoumarin (1b) and five closely related derivatives 1c-g were synthesized. In vitro evaluation with a catechol subunit for antioxidant and antimicrobial activity, these compounds using standard methods showed that compounds 1d, 1f displayed promise radical scavenging activity and 1f was found to be the most active one against Bacillus dysenteriae.
