Publication Type : Journal Article
Publisher : Journal of Enzyme Inhibition and Medicinal Chemistry
Source : Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 36, Issue 1, p.188-197 (2021)
Url : https://pubmed.ncbi.nlm.nih.gov/33430657/
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2021
Abstract : Nine compounds () containing the morpholine moiety were assessed for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Most of the compounds potently inhibited MAO-B; most potently inhibited with an IC value of 0.030 µM, followed by (0.25 µM). most potently inhibited AChE (IC = 6.1 µM), followed by (IC = 12.01 µM) and most potently inhibited MAO-A (IC = 7.1 µM). was a reversible mixed-type inhibitor of MAO-B ( = 0.018 µM); reversibly competitively inhibited AChE ( = 2.52 µM); and reversibly noncompetitively inhibited AChE ( = 7.04 µM). , and crossed the blood-brain barrier, and were non-toxic to normal VERO cells. These results show that is a selective inhibitor of MAO-B and that is a dual-acting inhibitor of AChE and MAO-B, and that both should be considered candidates for the treatment of Alzheimer's disease.
Cite this Research Publication : R. Sasidharan, Eom, B. Hyun, Heo, J. Hyun, Park, J. Eun, Abdelgawad, M. A., Musa, A., Gambacorta, N., Nicolotti, O., Manju, S. Leelabaiam, Bijo Mathew, and Kim, H., “Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations.”, Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 36, no. 1, pp. 188-197, 2021.