A Medical Approach to the Monoamine Oxidase Inhibition by Using 7Hbenzo[ e]perimidin-7-one Derivatives
Related Experiment Video
Updated: Mar 15, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Mitchell Bacho, Eduardo Coelho-Cerqueira, Cristian Follmer
1Laboratory of Pharmaceutical Chemistry, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Background:
A series of perimidinone derivatives (7H-benzo[e]perimidin-7-one) were synthesized and assessed by means of in vitro assays as human MAO inhibitors. These compounds inhibited reversibly the enzymes with inhibitory constants in the range of 2 to 20 μM. In addition, the selectivity of inhibition of the MAO isoforms seems to be significantly dependent of the presence either of heteroatom or electron donating and withdrawing groups on the perimidinone framework, which was verified by using molecular docking simulation with the crystallized MAO receptors. Most of these inhibitors were highly selective: 9 and 11 inhibited selectively the MAO-B isoform while 12 had 10-fold selectivity for MAO-A isoform. Moreover, the compound 12 was both the most selective and potent MAO-A inhibitor among perimidinones.
Result:
These results have important implications for the drug design of molecules targeting depression and movement-related disorders.
Related Concept Videos
Adrenergic Agonists: Indirect-Acting Agents
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Drugs Affecting Neurotransmitter Synthesis
Drugs Affecting Neurotransmitter Release or Uptake
Antidepressant Drugs: MAOIs and Other Agents
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...

