Makarian_2022_J.Mol.Struct_1247_

Reference

Title : Synthesis, kinetic evaluation and molecular docking studies of donepezil-based acetylcholinesterase inhibitors - Makarian_2022_J.Mol.Struct_1247_
Author(s) : Makarian M , Gonzalez M , Salvador SM , Lorzadeh S , Hudson PK , Pecic S
Ref : J Mol Struct , 1247 : , 2022
Abstract :

In an effort to develop new therapeutic agents to treat Alzheimer's disease, a series of donepezil-based analogs were designed, synthesized using an environmentally friendly route, and biologically evaluated for their inhibitory activity against electric eel acetylcholinesterase (AChE) enzyme. In vitro studies revealed that the phenyl moiety of donepezil can be successfully replaced with a pyridine ring leading to equally potent inhibitors of electric eel AChE. Further kinetic evaluations of the most potent inhibitor showed a dual-binding (mixed inhibition) mode, similar to donepezil. Molecular modeling studies suggest that several additional residues could be involved in the binding of this inhibitor in the human AChE enzyme active site compared to donepezil.

PubMedSearch : Makarian_2022_J.Mol.Struct_1247_
PubMedID: 35221376

Related information

Citations formats

Makarian M, Gonzalez M, Salvador SM, Lorzadeh S, Hudson PK, Pecic S (2022)
Synthesis, kinetic evaluation and molecular docking studies of donepezil-based acetylcholinesterase inhibitors
J Mol Struct 1247 :

Makarian M, Gonzalez M, Salvador SM, Lorzadeh S, Hudson PK, Pecic S (2022)
J Mol Struct 1247 :