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

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.