Bioorganic & Medicinal Chemistry Letters 2008-01-15

1-Aminoindanes as novel motif with potential atypical antipsychotic properties.

James M Graham, Linda L Coughenour, Bridget M Barr, David L Rock, Sham S Nikam

Index: Bioorg. Med. Chem. Lett. 18(2) , 489-93, (2008)

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Abstract

As part of an on-going effort to investigate the chemical space requirements for D(2)/5-HT(2A) 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 D(2), serotonin 5-HT(2A), and serotonin 5-HT(1A). Such compounds hold promise as a new chemical motif with atypical antipsychotic properties for the treatment of schizophrenia and related disorders.