Figures & data
Table 1 The IC50 values for the inhibition of recombinant human MAO-A and MAO-B by previously reported 2-acetylphenol analogs 1a–fCitation19
Table 2 The IC50 values for the inhibition of recombinant human MAO-A and MAO-B by 2-acetylphenol analogs 2a–o
Table 3 The IC50 values for the inhibition of recombinant human MAO-A and MAO-B by 2′,4′-dihydroxyacetophenone (4) and 2-acetylphenol derivatives 3a–b
Figure 1 Synthetic route to the 2-acetylphenol analogs 2a–o and 3a–b.
Note: Reagents and conditions: (a) acetone, K2CO3, reflux.
Figure 2 Reversibility of the inhibition of MAO-B by 2e.
Notes: MAO-B was preincubated in the absence of inhibitor (NI – dialyzed), in the presence of 2e (2e – dialyzed) and in the presence of the irreversible inhibitor, (R)-deprenyl (depr – dialyzed). These mixtures were subsequently dialyzed for 24 hours and the residual enzyme activity was measured. For comparison, the residual activity of undialyzed mixtures of MAO-B with 2e is also shown (2e – undialyzed).
Abbreviations: MAO, monoamine oxidase; h, hour.
Abbreviations: MAO, monoamine oxidase; h, hour.
Figure 3 Lineweaver–Burk graphs of human MAO-B activities in the absence (filled squares) and presence of various concentrations of 2e.
Notes: The concentrations of 2e used were equal to 1/4× IC50 (open squares), 1/2× IC50 (filled circles), 3/4× IC50 (open circles), 1× IC50 (triangles), 1 1/4× IC50 (diamonds). The insert is a graph of the slopes of the Lineweaver–Burk graphs versus inhibitor concentration.
Abbreviation: MAO, monoamine oxidase.
Abbreviation: MAO, monoamine oxidase.
