title: A Medical Approach to the Monoamine Oxidase Inhibition by Using 7Hbenzo[ e]perimidin-7-one Derivatives.
abstract: 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.
  
  
  RESULTS
  These results have important implications for the drug design of molecules targeting depression and movement-related disorders.
authors: Mitchell
authors: M
authors: Bacho
authors: Eduardo
authors: E
authors: Coelho-Cerqueira
authors: Cristian
authors: C
authors: Follmer
authors: Seyed Mohammad
authors: SM
authors: Nabavi
authors: Luca
authors: L
authors: Rastrelli
authors: Eugenio
authors: E
authors: Uriarte
authors: Laboratory of Pharmaceutical Chemistry, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain.
authors: Eduardo
authors: E
authors: Sobarzo-Sanchez
mesh_terms: D006801:Humans; D007700:Kinetics; D062105:Molecular Docking Simulation; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D008996:Monoamine Oxidase Inhibitors; D011799:Quinazolines; C022049:perimidine