Chasing ChEs-MAO B Multi-Targeting 4-Aminomethyl-7-Benzyloxy-2H-Chromen-2-ones
Copyright policy )Chasing ChEs-MAO B Multi-Targeting 4-Aminomethyl-7-Benzyloxy-2H-Chromen-2-ones
A series of 4-aminomethyl-7-benzyloxy-2H-chromen-2-ones was investigated with the aim of identifying multiple inhibitors of cholinesterases (acetyl- and butyryl-, AChE and BChE) and monoamine oxidase B (MAO B) as potential anti-Alzheimer molecules. Starting from a previously reported potent MAO B inhibitor (3), we studied single-point modifications at the benzyloxy or at the basic moiety. The in vitro screening highlighted triple-acting compounds (6, 8, 9, 16, 20) showing nanomolar and selective MAO B inhibition along with IC50 against ChEs at the low micromolar level. Enzyme kinetics analysis toward AChE and docking simulations on the target enzymes were run in order to get insight into the mechanism of action and plausible binding modes.
Monoamine Oxidase Inhibitors, Coumarin derivatives, Drug Evaluation, Preclinical, Structure-activity relationships, Molecular Dynamics Simulation, monoamine oxidase B inhibitors, Article, Structure-Activity Relationship, Coumarins, Monoamine oxidases B inhibitors, para-Aminobenzoates, Humans, Multitarget-directed ligands, Butyrylcholinesterase inhibitors, docking simulations, Molecular Structure, multi-target-directed ligands, coumarin derivatives, Enzyme Activation, Molecular Docking Simulation, Acetylcholinesterase inhibitors, acetylcholinesterase inhibitors, butyrylcholinesterase inhibitors, structure–activity relationships, Cholinesterase Inhibitors
Monoamine Oxidase Inhibitors, Coumarin derivatives, Drug Evaluation, Preclinical, Structure-activity relationships, Molecular Dynamics Simulation, monoamine oxidase B inhibitors, Article, Structure-Activity Relationship, Coumarins, Monoamine oxidases B inhibitors, para-Aminobenzoates, Humans, Multitarget-directed ligands, Butyrylcholinesterase inhibitors, docking simulations, Molecular Structure, multi-target-directed ligands, coumarin derivatives, Enzyme Activation, Molecular Docking Simulation, Acetylcholinesterase inhibitors, acetylcholinesterase inhibitors, butyrylcholinesterase inhibitors, structure–activity relationships, Cholinesterase Inhibitors
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