1-Aminoindanes as novel motif with potential atypical antipsychotic properties

As part of an on-going effort to investigate the chemical space requirements for D2/5-HT2A receptor antagonists as atypical antipsychotics, new 1-aminoindanes were synthesized. The replacement of the heterocycle (oxindole) in ziprasidone with a carbocycle (indane) was well tolerated and was found to retain binding affinities for dopamine D2, serotonin 5-HT2A, and serotonin 5-HT1A. Such compounds hold promise as a new chemical motif with atypical antipsychotic properties for the treatment of schizophrenia and related disorders.

As part of an on-going effort to investigate the chemical space requirements for D2/5-HT2A receptor antagonists as atypical antipsychotics, new 1-aminoindanes were synthesized. The replacement of the heterocycle (oxindole) in ziprasidone with a carbocycle (indane) was well tolerated and found to retain binding affinities for dopamine D2, serotonin 5-HT2A, and serotonin 5-HT1A receptors. Such compounds hold promise as a new chemical motif with atypical antipsychotic properties for the treatment of schizophrenia and related disorders.Figure optionsDownload as PowerPoint slide