[en] A set of 17 coumarin and 2 chromone derivatives with known inhibitory activity toward monoamine oxidase (MAO) A and B were tested as acetylcholinesterase (AChE) inhibitors. All compounds inhibited AChE with values in the micromolar range (3-100 microM). A kinetic study showed that most compounds acted as noncompetitive AChE inhibitors. This finding may be of interest in the context of Alzheimer's disease because recent observations suggest that MAO and AChE inhibition might decrease beta-amyloid deposition.
Disciplines :
Chemistry
Author, co-author :
Brühlmann, Corinne; Institut de Chimie Thérapeutique, Université de Lausanne, BEP, CH-1015 Lausanne, Switzerland
Ooms, Frédéric ; Université de Liège - ULiège > HEC Liège Research > HEC Liège Research: Strategy & Performance for the Society ; Institut de Chimie Thérapeutique, Université de Lausanne, BEP, CH-1015 Lausanne, Switzerland
Carrupt, Pierre-Alain; Institut de Chimie Thérapeutique, Université de Lausanne, BEP, CH-1015 Lausanne, Switzerland
Testa, Bernard; Institut de Chimie Thérapeutique, Université de Lausanne, BEP, CH-1015 Lausanne, Switzerland
Catto, Marco; Dipartimento Farmaco-Chimico, Università di Bari, I-70125 Bari, Italy
Leonetti, Francesco; Dipartimento Farmaco-Chimico, Università di Bari, I-70125 Bari, Italy
Altomare, Cosimo; Dipartimento Farmaco-Chimico, Università di Bari, I-70125 Bari, Italy
Carotti, Angelo; Dipartimento Farmaco-Chimico, Università di Bari, I-70125 Bari, Italy
Language :
English
Title :
Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase.
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