213664-68-7Relevant articles and documents
1,3-Disubstituted benzazepines as neuropeptide Y Y1 receptor antagonists
Murakami, Yasushi,Hagishita, Sanji,Okada, Tetsuo,Kii, Makoto,Hashizume, Hiroshi,Yagami, Tatsuroh,Fujimoto, Masafumi
, p. 1703 - 1714 (2007/10/03)
A novel class of potent and selective non-peptide neuropeptide Y (NPY) Y1 receptor antagonists, having benzazepine nuclei, have been designed, synthesized, and evaluated for activity. Through a blind screening we found the compound 1-N-(3-(N' -(tert-butoxycarbonyl)amino)benzyl)-7-methoxy-3-(3)-methylureido)-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one (9: IC50 =1.6 μM). Chemical modifications of 9 gave a potent NPY Y1 antagonist 3-(N-(4-hydroxyphenyl)-N0 -methylguanidino)-1-N-(3-(N'-(tert- butoxycarbonyl)amino)benzyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one (14c: IC50 =43 nM), which had no affnity for NPY Y2 and Y5 receptors. (C) 1999 Elsevier Science Ltd. All rights reserved.