Potential of Vitamin B6 Dioxime Analogues to Act as Cholinesterase Ligands.

ABSTRACT: Seven pyridoxal dioxime quaternary salts (1-7) were synthesized with the aim of studying their interactions with human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The synthesis was achieved by the quaternization of pyridoxal monooxime with substituted 2-bromoacetophenone oximes (phenacyl bromide oximes). All compounds, prepared in good yields (43-76%) and characterized by 1D and 2D NMR spectroscopy, were evaluated as reversible inhibitors of cholinesterase and/or reactivators of enzymes inhibited by toxic organophosphorus compounds. Their potency was compared with that of their monooxime analogues and medically approved oxime HI-6. The obtained pyridoxal dioximes were relatively weak inhibitors for both enzymes (K_i = 100-400 µM). The second

SUBMITTER: Gaso Sokac D 

PROVIDER: S-EPMC9655973 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature