We report the discovery and the synthesis of novel, potential antipsychotic compounds combining potent dopamine D2 receptor antagonist and serotonin 5-HT1A receptor agonist properties in the same molecule. We describe the structure-activity relationship that lead us to the promising derivative: N-[(2, 2-dimethyl-2, 3-dihydro-benzofuran-7-yloxy) ethyl]-3- (cyclopent-1-enyl)-benzylamine 16. The latter has high affinity for D2 and 5-HT1A ...