Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

Authors
Beck, JP Arvanitis, AG Curry, MA Rescinito, JT Fitzgerald, LW Gilligan, PJ Zaczek, R Trainor, GL
Citation
Jp. Beck et al., Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists, BIOORG MED, 9(7), 1999, pp. 967-972
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
7
Year of publication
1999
Pages
967 - 972
Database
ISI
SICI code
0960-894X(19990405)9:7<967:PACH(R>2.0.ZU;2-4
Abstract
A series of purin-8-ones was prepared and discovered to have excellent bind ing affintity to the CRH-R1 receptor. Structure-activity studies focused on amine side-chain optimization, urea substitution and pyridyl isostere inco rporation. Thus, the highly potent purin-8-ones show promise as a new class of potential anxiolytics and/or antidepressants. (C) 1999 DuPont Pharmaceu ticals. Published by Elsevier Science I,td. All rights reserved.