Substituted xanthones as selective and reversible monoamine oxidase A (MAO-A) inhibitors.
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).
Thull
U
U
Institut de chimie thérapeutique, Ecole de Pharmacie, Université de Lausanne, Switzerland.
Kneubühler
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S
Testa
B
B
Borges
M F
MF
Pinto
M M
MM
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
D008996:Monoamine Oxidase Inhibitors; D009419:Nerve Tissue Proteins; D014970:Xanthines; D008995:Monoamine Oxidase