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A new series of 3-phenylcoumarins as potent and selective MAO-B inhibitors.
Matos, Maria Joao; Viña, Dolores; Quezada, Elias; Picciau, Carmen; Delogu, Giovanna; Orallo, Francisco; Santana, Lourdes; Uriarte, Eugenio.
Afiliação
  • Matos MJ; Departamento de Química Orgánica, Facultad de Farmacia, 15782 Santiago de Compostela, Spain. mariacmatos@gmail.com
Bioorg Med Chem Lett ; 19(12): 3268-70, 2009 Jun 15.
Article em En | MEDLINE | ID: mdl-19423346
ABSTRACT
6-Methyl-3-phenylcoumarins 3-6 were designed, synthesized and evaluated as monoamine oxidase A and B (MAO-A and MAO-B) inhibitors. The synthesis of these new compounds (resveratrol-coumarin hybrids) was carried out with good yield by a Perkin reaction, from the 5-methylsalicylaldehyde and the corresponding phenylacetic acid. They show high selectivity to the MAO-B isoenzyme, with IC(50) values in the nanomolar range. Compound 5 is the most active compound and is several times more potent and selective than the reference compound, R-(-)-deprenyl.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Estilbenos / Cumarínicos / Inibidores da Monoaminoxidase Idioma: En Ano de publicação: 2009 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Estilbenos / Cumarínicos / Inibidores da Monoaminoxidase Idioma: En Ano de publicação: 2009 Tipo de documento: Article