1134396-07-8Relevant articles and documents
Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity
Guan, Liping,Jia, Jinjing,Jiang, Haiying,Peng, Dingxin,Zhang, Li
supporting information, (2021/10/01)
The marine environment is a rich resource for discovering functional materials, and seaweed is recognized for its potential use in biology and medicine. Liquiritigenin has been isolated and identified from Sargassum pallidum. To find new anti-Alzheimer's activity, we designed and synthesized thirty-two 7-prenyloxy-2,3-dihydroflavanone derivatives (3a-3p) and 5-hydroxy-7-prenyloxy-2,3-dihydro-flavanone derivatives (4a-4p) as cholinesterases inhibitors based on liquiritigenin as the lead compound. Inhibition screening against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) indicated that all synthesized compounds possessed potent AChE inhibitory activity and moderated to weak BuChE inhibitory activity in vitro. Kinetic studies demonstrated that compound 4o inhibited AChE via a dual binding site ability. In addition, all compounds displayed the radical scavenging effects. Finally, the molecular docking simulation of 4o in AChE active site displayed good agreement with the obtained the pharmacological results.
Synthesis and studies on antidepressant effect of 5,7-Dihydroxyflavanone derivatives
Zhao, Dong-Hai,Sui, Xin,Qu, You-Le,Yang, Li-Ye,Wang, Xian,Guan, Li-Ping
, p. 1129 - 1132 (2011/12/16)
A series of 5,7-dihydroxyflavanone derivatives were synthesized and evaluated their antidepressant activities. The results showed that of nine compounds significantly reduced times during the forced swimming test at a dose of 10 mg/kg, indicative of antidepressant activity. Among the compounds, 4o (4'-methoxy-5,7,3'-trihydroxyflavanone) was found to be the most potent and it was observed that the compound 4o at dose of 10, 20 and 40 mg/kg significantly reduced the duration of immobility times in the Forced swimming test in mice 0.5 h after treatment.