Title : Synthesis, Molecular Docking, and Biological Evaluation of Benzimidazole Derivatives as Selective Butyrylcholinesterase Inhibitors - Ha_2021_Curr.Alzheimer.Res__ |
Author(s) : Ha ZY , Ong HC , Oo CW , Yeong KY |
Ref : Curr Alzheimer Res , : , 2021 |
Abstract :
Benzimidazole is an interesting pharmacophore, and its derivatives have been previously shown to possess cholinesterase inhibitory activity. In this study, benzimidazole derivatives were synthesized via a 4-step reaction scheme and screened for their acetylcholinesterase and butyrylcholinesterase inhibitory activities. Among the synthesised compounds, three of them (5IIa, 5IIb, and 5IIc) exhibited potent, selective butyrylcholinesterase inhibition at a low micromolar level. The compounds did not show any significant cytotoxicity when tested against a panel of human cell lines. Moreover, the most active compound, 5IIc, was highly permeable across the blood-brain barrier. The structure-activity relationship and molecular interactions of the synthesized benzimidazole derivatives were also analysed and discussed. |
PubMedSearch : Ha_2021_Curr.Alzheimer.Res__ |
PubMedID: 33602088 |
Ha ZY, Ong HC, Oo CW, Yeong KY (2021)
Synthesis, Molecular Docking, and Biological Evaluation of Benzimidazole Derivatives as Selective Butyrylcholinesterase Inhibitors
Curr Alzheimer Res
:
Ha ZY, Ong HC, Oo CW, Yeong KY (2021)
Curr Alzheimer Res
: