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ID: ALA1147765

Journal: Bioorg Med Chem Lett

Title: Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.

Authors: Ceccarelli SM, Pinard E, Stalder H, Alberati D.

Abstract: During SAR exploration of N-(2-aryl-cyclohexyl) substituted spiropiperidine as GlyT1 inhibitors, it was found that introduction of an hydroxy group in position 2 of the cyclohexyl residue considerably improves the pharmacological profile. In particular, reduction of the binding affinity at the nociceptin/orphanin FQ peptide and the mu opioid receptors was achieved.

CiteXplore: 16246561

DOI: 10.1016/j.bmcl.2005.09.067