Title : Design and synthesis of ligustrazine derivatives as potential anti-Alzheimer's agents - Chen_2023_Nat.Prod.Res__1 |
Author(s) : Chen XF , Li SS , Bai YJ , Zhao ZF , Gong G , He XR , Zheng XH |
Ref : Nat Prod Res , :1 , 2023 |
Abstract :
A novel series of ligustrazine derivatives was designed, synthesized, and evaluated as acetylcholinesterase (AChE) and butylcholinesterase (BuChE) inhibitors for the treatment of Alzheimer's disease (AD). In vitro studies displayed that some of the synthesized compounds revealed promising AChE and BuChE inhibitory effects. Particularly, compounds E12 and E27, indicated highly AChE inhibitory activity with IC(50) values of 1.85 microM and 0.98 microM, respectively and showed noteworthy protective effects against on glutamate-induced SH-SY5Y cells damage at 1 microM and 10 microM concentrations. Furthermore, molecular simulation docking elucidates compounds E12 and E27 interacting with residues in the binding site of AChE (PDB code: 4EY7) and BuChE (PDB code: 1P0I), emphasizing the protein residues that participate in the main interactions with the two targets. Taken together, these results revealed that compounds E12 and E27 might be potential lead compounds for further structure optimization in the drug-discovery process against AD. |
PubMedSearch : Chen_2023_Nat.Prod.Res__1 |
PubMedID: 37505222 |
Chen XF, Li SS, Bai YJ, Zhao ZF, Gong G, He XR, Zheng XH (2023)
Design and synthesis of ligustrazine derivatives as potential anti-Alzheimer's agents
Nat Prod Res
:1
Chen XF, Li SS, Bai YJ, Zhao ZF, Gong G, He XR, Zheng XH (2023)
Nat Prod Res
:1