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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.

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  • 1Chemical & Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA.


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.

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