Substituted Xanthones as Selective and Reversible Monoamine Oxidase A (MAO-A) Inhibitors |
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| Authors: | Thull Ulrike Kneubühler Silvia Testa Bernard Borges M Fernanda M Pinto Madalena M M |
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| Institution: | (1) Institut de chimie thérapeutique, Ecole de Pharmacie, Université de Lausanne, CH-1015 Lausanne, Switzerland;(2) Laboratorio de Química Orgânica, Faculdade de Farmácia do Porto, P-4000 Porto, Portugal |
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| Abstract: | l,3-Dihydroxy-2-methylxanthone (XI), its 4-chloro and 4-bromo derivatives (X1-C1 and Xl-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 XI displaying the highest activity (IC50 = 3.7 µM). |
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| Keywords: | dihydroxymethylxanthones monoamine oxidase (MAO) MAO-A selective reversible inhibitors |
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