Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase.
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.
Brühlmann
C
C
Institut de Chimie Thérapeutique, Université de Lausanne, BEP, CH-1015 Lausanne, Switzerland.
Ooms
F
F
Carrupt
P A
PA
Testa
B
B
Catto
M
M
Leonetti
F
F
Altomare
C
C
Carotti
A
A
D000110:Acetylcholinesterase / Q000737:chemistry; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry; D004524:Eels; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D003374:Coumarins; D008996:Monoamine Oxidase Inhibitors; D000110:Acetylcholinesterase