DUAL CCK-A AND CCK-B RECEPTOR ANTAGONISTS .1. C9-METHYL-1,4-BENZODIAZEPINES

Authors
TABUCHI S ITO H SOGABE H KUNO M KATSUMI I YAMAMOTO N MITSUI H SATOH Y
Citation
S. Tabuchi et al., DUAL CCK-A AND CCK-B RECEPTOR ANTAGONISTS .1. C9-METHYL-1,4-BENZODIAZEPINES, Bioorganic & medicinal chemistry letters, 7(2), 1997, pp. 169-174
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
2
Year of publication
1997
Pages
169 - 174
Database
ISI
SICI code
0960-894X(1997)7:2<169:DCACRA>2.0.ZU;2-0
Abstract
A novel series of potent CCK-A and CCK-B dual antagonists has been pre pared which incorporate a methyl substituent at the 9 position of a 1, 4-benzodiazepine ring system. FR193108 ((+)-11) was selected for furth er biological evaluation, and is expected to be more efficacious than CCK-A selective antagonists for the treatment of pancreatitis, since i t has high and well-balanced affinities for both CCK-A and -B receptor s. (C) 1997, Elsevier Science Ltd.