Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics

A series of 3-aminoethyl-1-tetralones, conformationally constrained higher homologues of haloperidol (standard for typical antipsychotic profile), have been obtained by a four-step route from valerolactone. Their binding affinities at dopamine D2 and serotonin 5-HT2A and 5-HT2C receptors were determined, showing in some cases an atypical antipsychotic profile.

Graphical abstractThe preparation and binding affinities of new 3-aminoethyl-1-tetralones are reported. Some of these compounds (e.g., 6) showed potential atypical antipsychotic profiles.Figure optionsDownload full-size imageDownload as PowerPoint slide