1, 3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists

…, T Okada, H Hashizume, M Kii, Y Ishihara…

Index: Murakami, Yasushi; Hara, Hirokazu; Okada, Tetsuo; Hashizume, Hiroshi; Kii, Makoto; Ishihara, Yasunobu; Ishikawa, Michio; Shimamura, Mayumi; Mihara, Shin-Inchi; Kato, Goro; Hanasaki, Kohji; Hagishita, Sanji; Fujimoto, Masafumi Journal of Medicinal Chemistry, 1999 , vol. 42, # 14 p. 2621 - 2632

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Citation Number: 54

Abstract

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-( ...