Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPCsynthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179)

Authors
Einsiedel, J Hubner, H Gmeiner, P
Citation
J. Einsiedel et al., Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPCsynthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179), BIOORG MED, 11(18), 2001, pp. 2533-2536
Citations number
34
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
18
Year of publication
2001
Pages
2533 - 2536
Database
ISI
SICI code
0960-894X(20010917)11:18<2533:BBIDSE>2.0.ZU;2-8
Abstract
Conformationally restricted benzamide bioisosteres were investigated when t he chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (K-ihigh=0.95nM). Mitogenesi s experiments indicated partial agonist properties (42%). EPC syntheses of the target compounds of type 4 were performed starting from alpha -amino ac ids. (C) 2001 Elsevier Science Ltd. All rights reserved.