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ID: ALA1138975

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.

Authors: Alberati D, Ceccarelli SM, Jolidon S, Krafft EA, Kurt A, Maier A, Pinard E, Stalder H, Studer D, Thomas AW, Zimmerli D.

Abstract: A novel class of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-ones have been discovered and developed as potent and selective GlyT1 inhibitors. The molecules are devoid of activity at the GlyT2 isoform and display excellent selectivities against the mu opioid receptor as well as the nociceptin/orphanin FQ peptide (NOP) receptor. A novel, straightforward and efficient synthetic strategy for the assembly of the target molecules is also presented.

CiteXplore: 16762548

DOI: 10.1016/j.bmcl.2006.05.064