Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists

A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K+ channel and serotonin transporter.

Graphical abstractIdentification and detailed SAR of a novel series of cyclohexanamine derivatives as potent neuropeptide Y Y1 ligands are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide