1-Aminoindanes as novel motif with potential atypical antipsychotic properties

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 found to r...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-01, Vol.18 (2), p.489-493
Hauptverfasser: Graham, James M., Coughenour, Linda L., Barr, Bridget M., Rock, David L., Nikam, Sham S.
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Sprache:eng
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Zusammenfassung: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 found to retain binding affinities for dopamine D 2, serotonin 5-HT 2A, and serotonin 5-HT 1A receptors. 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 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.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2007.11.106