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Peer-reviewed veterinary case report

Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2009
Authors:
Caldwell, John P et al.
Affiliation:
CV & CNS Department of Chemical Research · United States

Abstract

A series of N-8 substituted analogs based upon the spiropiperidine core of the original lead compound 1 was synthesized. This lead has been elaborated to compounds to give compounds 2 and 3 (R=H) that exhibited high NOP binding affinity as well as selectivity against other known opioid receptors. These two series have been further functionalized at the amido nitrogen. The synthesis and structure-activity relationship (SAR) of these and related compounds are discussed.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/19147350/