A novel series of potent and selective non-peptide neuropeptide Y (NPY) Y1 receptor antagonists, having benzazepine nuclei, have been designed, synthesized, and evaluated for activity. Chemical modification of the R1 and R3 substituents in structure 1 (Chart 1) yields several compounds that show high affinity for the Y1 receptor (K i values of less than 10 nM). SAR studies revealed that introduction of an isopropylurea group at R1 and a 3-( ...
