Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations

Nine compounds (MO1–MO9) containing the morpholine moiety were assessed for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Most of potently inhibited MAO-B; MO1 most with an IC50 value 0.030 µM, followed by MO7 (0.25 µM). MO5 AChE (IC50 = 6.1 µM), MO9 12.01 µM) MAO-A 7.1 was a reversible mixed-type inhibitor MAO-B (Ki 0.018 µM); reversibly competitively 2.52 noncompetitively 7.04 MO1, crossed blood–brain barrier, non-toxic to normal VERO cells. These results show that is selective dual-acting MAO-B, both should be considered candidates treatment Alzheimer’s disease.