title: Substituted xanthones as selective and reversible monoamine oxidase A (MAO-A) inhibitors.
abstract: 1,3-Dihydroxy-2-methylxanthone (X1), its 4-chloro and 4-bromo derivatives (X1-Cl and X1-Br), and 1,3-dihydroxy-4-methylxanthone were investigated for their inhibition activities toward MAO. A hyperbolic function was derived to fit the data and to calculate IC50 values. The compounds proved to be reversible and selective inhibitors of MAO-A, with X1 displaying the highest activity (IC50 = 3.7 microM).
authors.affiliation: Institut de chimie thérapeutique, Ecole de Pharmacie, Université de Lausanne, Switzerland.
authors.forename: U
authors.initials: U
authors.lastname: Thull
authors.forename: S
authors.initials: S
authors.lastname: Kneubühler
authors.forename: B
authors.initials: B
authors.lastname: Testa
authors.forename: M F
authors.initials: MF
authors.lastname: Borges
authors.forename: M M
authors.initials: MM
authors.lastname: Pinto
mesh_terms: D000818:Animals; D001921:Brain / Q000648:ultrastructure; D001923:Brain Chemistry / Q000187:drug effects; D066298:In Vitro Techniques; D007700:Kinetics; D008928:Mitochondria / Q000187:drug effects / Q000201:enzymology; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D009419:Nerve Tissue Proteins / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D014970:Xanthines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D008996:Monoamine Oxidase Inhibitors; D009419:Nerve Tissue Proteins; D014970:Xanthines; D008995:Monoamine Oxidase