CCKB SELECTIVE RECEPTOR LIGANDS - NOVEL 1,3,5-TRISUBSTITUTED BENZAZEPIN-2-ONES

Authors
VANNIEL MB FREEDMAN SB MATASSA VG PATEL S PENGILLEY RR SMITH AJ
Citation
Mb. Vanniel et al., CCKB SELECTIVE RECEPTOR LIGANDS - NOVEL 1,3,5-TRISUBSTITUTED BENZAZEPIN-2-ONES, Bioorganic & medicinal chemistry letters, 5(13), 1995, pp. 1421-1426
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
13
Year of publication
1995
Pages
1421 - 1426
Database
ISI
SICI code
0960-894X(1995)5:13<1421:CSRL-N>2.0.ZU;2-H
Abstract
The novel 3-ureidobenzazepin-2-ones 11 and 12, which incorporate a cat ionic substituent at the 5-position were designed and synthesised as l igands for the CCKB receptor. These compounds proved to have high affi nity for the CCKB receptor and were selective over the CCKA receptor s ubtype. This work further defines the role of the benzazepine template as a bioisostere for the 1,4-benzodiazepine template of earlier CCK a ntagonists.