108238-40-0Relevant articles and documents
Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities
Luo, Wen,Chen, Ying,Wang, Ting,Hong, Chen,Chang, Li-Ping,Chang, Cong-Cong,Yang, Ya-Cheng,Xie, Song-Qiang,Wang, Chao-Jie
, p. 672 - 680 (2016)
A novel series of 7-aminoalkyl-substituted flavonoid derivatives 5a-5r were designed, synthesized and evaluated as potential cholinesterase inhibitors. The results showed that most of the synthesized compounds exhibited potent acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities at the micromolar range. Compound 2-(naphthalen-1-yl)-7-(8-(pyrrolidin-1-yl)octyloxy)-4H-chromen-4-one (5q) showed the best inhibitory activity (IC50, 0.64 μM for AChE and 0.42 μM for BChE) which were better than our previously reported compounds and the commercially available cholinergic agent Rivastigmine. The results from a Lineweaver-Burk plot indicated a mixed-type inhibition for compound 5q with AChE and BChE. Furthermore, molecular modeling study showed that 5q targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, these compounds (5a-5r) did not affect PC12 and HepG2 cell viability at the concentration of 10 μM. Consequently, these flavonoid derivatives should be further investigated as multipotent agents for the treatment of Alzheimer's disease.
Cleavage of methyl ethers of flavones by chloroaluminate ionic liquid
Liu, Tao,Hu, Yongzhou
, p. 3209 - 3218 (2007/10/03)
A new o-demethylation method of a series of mono-, di-, trimethoxy-flavones using a chloroaluminate ionic liquid - [BMIM] [Al2Cl7] in dichloromethane is described. The desired products were obtained in moderate to good yields.