| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365354 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
Graphical abstractAs 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 full-size imageDownload as PowerPoint slide
