Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase

Citation
C. Bruhlmann et al., Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase, J MED CHEM, 44(19), 2001, pp. 3195-3198
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
44
Issue
19
Year of publication
2001
Pages
3195 - 3198
Database
ISI
SICI code
0022-2623(20010913)44:19<3195:CDADIO>2.0.ZU;2-C
Abstract
A set of 17 coumarin and 2 chromone derivatives with known inhibitory activ ity toward monoamine oxidase (MAO) A and B were tested as acetylcholinester ase (ACNE) inhibitors. All compounds inhibited ACNE with values in the micr omolar range (3-100 muM). A kinetic study showed that most compounds acted as noncompetitive ACNE inhibitors. This finding may be of interest in the c ontext of Alzheimer's disease because recent observations suggest that MAO and ACNE inhibition might decrease beta -amyloid deposition.