期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 12, 页码 3268-3270出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.085
关键词
Coumarin; Resveratrol; Monoamino oxidase inhibitors; Perkin reaction; 3-Phenylcoumarins
资金
- Spanish Ministerio de Sanidad y Consumo [PI061457, PI061537]
- Xunta da Galicia [PXIB20304PR, INCITE08PXIB203022PR, 08CSA019203PR]
- Fondazione Banco Sardegna (Italy)
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. (C) 2009 Elsevier Ltd. All rights reserved.
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