Piperazinyl benzamidines: Synthesis and affinity for the delta opioid receptor

Authors
Nortey, SO Baxter, EW Codd, EE Zhang, SP Reitz, AB
Citation
So. Nortey et al., Piperazinyl benzamidines: Synthesis and affinity for the delta opioid receptor, BIOORG MED, 11(13), 2001, pp. 1741-1743
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
13
Year of publication
2001
Pages
1741 - 1743
Database
ISI
SICI code
0960-894X(20010709)11:13<1741:PBSAAF>2.0.ZU;2-O
Abstract
Piperazinyl benzamidines were prepared and found to bind to the rat delta ( delta) opioid receptor. The most active compounds had a N,N-diethylcarboxam ido group and N-benzyl piperazine. The most potent among these was N,N-diet hyl-4-[4-(phenylmethyl)-1 -piperazinyl][2-(trifluoromethyl)phenyl]iminometh yl]benzamide (27) with a 1.22 nM K-i for the rat delta opioid receptor and ca. 1000x selectivity relative to the mu opioid subtype. (C) 2001 Elsevier Science Ltd. All rights reserved.