Details

Autor(en) / Beteiligte

• Matos, Maria Joao
• Viña, Dolores
• Quezada, Elias
• Picciau, Carmen
• Delogu, Giovanna
• Orallo, Francisco
• Santana, Lourdes
• Uriarte, Eugenio

Titel

A new series of 3-phenylcoumarins as potent and selective MAO-B inhibitors

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2009-06, Vol.19 (12), p.3268-3270

Ort / Verlag

Amsterdam: Elsevier Ltd

Erscheinungsjahr

2009

Quelle

MEDLINE

Beschreibungen/Notizen

• 6-Methyl-3-phenylcoumarins 3–6 were design, 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. 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.