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.