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    Bioorg Med Chem Lett. 2009 Feb 15;19(4):1115-7. doi: 10.1016/j.bmcl.2008.12.107. Epub 2009 Jan 3.

    Identification of a series of benzoxazoles as potent 5-HT6 ligands.

    Liu KG, Lo JR, Comery TA, Zhang GM, Zhang JY, Kowal DM, Smith DL, Di L, Kerns EH, Schechter LE, Robichaud AJ.

    Source

    Chemical & Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA. liuk1@wyeth.com

    Abstract

    As part of our continuing efforts to identify therapeutics for CNS diseases such as schizophrenia and Alzheimer's disease (AD), we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands as a potential treatment for cognitive dysfunction. Herein we report the identification of a novel series of benzoxazole derivatives as potent 5-HT(6) ligands. The synthesis and detailed SAR of this class of compounds are reported. The compounds have been shown to be full antagonists in a cyclic AMP functional assay.

    PMID:
    19152787
    [PubMed - indexed for MEDLINE]

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