3-Substituted coumarins as dual inhibitors of AChE and MAO for the treatment of Alzheimer's disease

The complex etiology of Alzheimer's disease (AD) has encouraged active research in the development of multi-target drugs with two or more complementary biological activities, since they may represent an important advance in the treatment of this disease. A series of 3-substituted coumarins were...

Full description

Saved in:
Bibliographic Details
Published in:MedChemComm 2012-02, Vol.3 (2), p.213-218
Main Authors: Via, Dolores, Matos, Maria Joo, Yez, Matilde, Santana, Lourdes, Uriarte, Eugenio
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The complex etiology of Alzheimer's disease (AD) has encouraged active research in the development of multi-target drugs with two or more complementary biological activities, since they may represent an important advance in the treatment of this disease. A series of 3-substituted coumarins were synthesized and evaluated as monoamino oxidases (MAO) and acetylcholinesterase (AChE) inhibitors. Most of the 3-benzamide coumarin derivatives inhibited both MAO-B and AChE with values in the micromolar range. It might be a promising direction for developing novel drugs as potential agents for the treatment of AD patients. Three series of 3-substituted coumarin derivatives have been synthesized and evaluated as dual hMAO/hAChE inhibitors. The importance of the substituents in that position is determined.
ISSN:2040-2503
2040-2511
DOI:10.1039/c1md00221j