A new series of 3-phenylcoumarins as potent and selective MAO-B inhibitors.
Article Details
- CitationCopy to clipboard
Matos MJ, Vina D, Quezada E, Picciau C, Delogu G, Orallo F, Santana L, Uriarte E
A new series of 3-phenylcoumarins as potent and selective MAO-B inhibitors.
Bioorg Med Chem Lett. 2009 Jun 15;19(12):3268-70. doi: 10.1016/j.bmcl.2009.04.085. Epub 2009 Apr 24.
- PubMed ID
- 19423346 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Iproniazid Amine oxidase [flavin-containing] B IC 50 (nM) 7540 N/A N/A Details Selegiline Amine oxidase [flavin-containing] A IC 50 (nM) 67250 N/A N/A Details Selegiline Amine oxidase [flavin-containing] B IC 50 (nM) 19.6 N/A N/A Details