Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists

Authors
Luthin, DR Rabinovich, AK Bhumralkar, DR Youngblood, KL Bychowski, RA Dhanoa, DS May, JM
Citation
Dr. Luthin et al., Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists, BIOORG MED, 9(5), 1999, pp. 765-770
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
765 - 770
Database
ISI
SICI code
0960-894X(19990308)9:5<765:SABAOO>2.0.ZU;2-B
Abstract
A novel series of derivatives of oxo-7H-benzo[e]perimidine-4-carboxylic aci d (I) potently displaced radioligand binding of I-125-CRF to both CRF1 and CRF2 receptors. The members of this series antagonized CRF-stimulated cAMP formation and CRF-stimulated corticotropin release from rat pituitary in vi vo. These are the first nonpeptide antagonists to show activity at both CRF 1 and CRF2 receptors. (C) 1999 Elsevier Science Ltd. All rights reserved.