5,7-DIPHENYL-3-UREIDOHEXAHYDROAZEPIN-2-ONES CHOLECYSTOKININ-B RECEPTOR LIGANDS

Authors
LOWE JA QIAN WM SCOTT PJ MCLEAN S BRYCE DK CRAWFORD RT BORDNER J
Citation
Ja. Lowe et al., 5,7-DIPHENYL-3-UREIDOHEXAHYDROAZEPIN-2-ONES CHOLECYSTOKININ-B RECEPTOR LIGANDS, Bioorganic & medicinal chemistry letters, 4(24), 1994, pp. 2877-2882
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
24
Year of publication
1994
Pages
2877 - 2882
Database
ISI
SICI code
0960-894X(1994)4:24<2877:5CR>2.0.ZU;2-D
Abstract
A series of 5,7-diphenyl-3-ureidohexahydroazepin-2-one cholecystokinin -B (CCK-B) receptor antagonists was synthesized using Beckmann ring ex pansion of a suitable 2,4-diphenylcyclohexanone as a key step. SAR stu dies revealed the importance of the 5-aryl group for high and selectiv e CCK-B receptor affinity, as illustrated in compound(-)10i (CCK-B IC5 0 = 6.8 nM).