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 |
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Format: | Artikel |
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. |
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ISSN: | 0960-894X 0968-0896 1464-3405 1464-3391 |
DOI: | 10.1016/j.bmcl.2007.11.106 |