| Title : Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease - Wu_2021_Bioorg.Med.Chem.Lett__128316 |
| Author(s) : Wu J , Kou X , Ju H , Zhang H , Yang A , Shen R |
| Ref : Bioorganic & Medicinal Chemistry Lett , :128316 , 2021 |
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Abstract :
A series of naringenin derivatives were designed and synthesized as multifunctional anti-Alzheimer's disease (AD) agents. The results showed that these derivatives displayed moderate-to-good acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities at the micromolar range (IC(50), 12.91-62.52 microM for AChE and 0.094-13.72 microM for BuChE). Specifically, compound 1 showed the highest inhibitory activity against BuChE with the IC(50) value of (0.094+/-0.0054) microM. A Lineweaver-Burk plot and molecular docking studies demonstrated that 1 targeted both the catalytically active site (CAS) and the peripheral anion site (PAS) of BuChE. Besides, all derivatives showed excellent hydroxyl free radicals (.OH) scavenging ability than vitamin C and cyclic voltammetry results displayed that 1 could effectively scavenge superoxide anion radical (.O(2)(-)). In addition, compound 1 displayed good metal chelating properties and had anti-Abeta aggregation activities. Therefore, compound 1 might be the potential anti-AD agent for further developments. |
| PubMedSearch : Wu_2021_Bioorg.Med.Chem.Lett__128316 |
| PubMedID: 34391893 |
Wu J, Kou X, Ju H, Zhang H, Yang A, Shen R (2021)
Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease
Bioorganic & Medicinal Chemistry Lett
:128316
Wu J, Kou X, Ju H, Zhang H, Yang A, Shen R (2021)
Bioorganic & Medicinal Chemistry Lett
:128316