SAR STUDY OF THE INDOLE MOIETY OF CI-988, A POTENT AND SELECTIVE CCK-B ANTAGONIST

Authors
AUGELLISZAFRAN CE PURCHASE TS ROTH BD TAIT B TRIVEDI BK WILSON M SUMANCHAUHAN N WEBDALE L
Citation
Ce. Augelliszafran et al., SAR STUDY OF THE INDOLE MOIETY OF CI-988, A POTENT AND SELECTIVE CCK-B ANTAGONIST, Bioorganic & medicinal chemistry letters, 7(15), 1997, pp. 2009-2014
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
15
Year of publication
1997
Pages
2009 - 2014
Database
ISI
SICI code
0960-894X(1997)7:15<2009:SSOTIM>2.0.ZU;2-R
Abstract
Due to the interesting pharmacological activity observed for CI-988, a potent and selective CCK-B receptor antagonist, we have continued to study the SAR of this antagonist. This particular study examines the i mportance of the indole moiety for binding affinity. The synthesis and receptor binding affinity for analogs containing functionalized indol e derivatives and replacing the indole with various heterocycles are r eported. (C) 1997 Elsevier Science Ltd.