Structure-activity relationships of neuropeptide YY1 receptor antagonists related to BIBP 3226

Authors
Aiglstorfer, I Hendrich, I Moser, C Bernhardt, G Dove, S Buschauer, A
Citation
I. Aiglstorfer et al., Structure-activity relationships of neuropeptide YY1 receptor antagonists related to BIBP 3226, BIOORG MED, 10(14), 2000, pp. 1597-1600
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
14
Year of publication
2000
Pages
1597 - 1600
Database
ISI
SICI code
0960-894X(20000717)10:14<1597:SRONYR>2.0.ZU;2-D
Abstract
Analogues of BIBP 3226, (R)-N-alpha-diphenylacetyl-N-(4-hydroxybenzyl)argin inamide, were synthesized and investigated for Y-1 antagonism (Ca2+-assay, HEL cells) and binding on Y-1, Y-2 and Y-5 receptors. Replacing the benzyla mino by a tetrahydrobenzazepinyl group preserves most of the Y-1 activity. Combination with a N-G-phenylpropyl arginine and a N-alpha-p-biphenyly-lace tyl moiety shifted the NPY receptor selectivity towards Y-5 (C) 2000 Elsevi er Science Ltd. All rights reserved.