Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists

Authors
Zarrinmayeh, H Zimmerman, DM Cantrell, BE Schober, DA Bruns, RF Gackenheimer, SL Ornstein, PL Hipskind, PA Britton, TC Gehlert, DR
Citation
H. Zarrinmayeh et al., Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists, BIOORG MED, 9(5), 1999, pp. 647-652
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
647 - 652
Database
ISI
SICI code
0960-894X(19990308)9:5<647:SROASO>2.0.ZU;2-M
Abstract
A series of benzimidazoles (4) was synthesized and evaluated in vitro as po tent and selective NPY Y1 receptor antagonists. Substitution of the piperid ine nitrogen of 4 with appropriate R groups resulted in compounds with more than 80-fold higher affinity at the Y1 receptor compared to the parent com pound 5 (R = H). The most potent benzimidazole in this series was 21 (K-i = 0.052 nM). (C) 1999 Elsevier Science Ltd. All rights reserved.