4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D-4 receptors

Authors
Moore, KW Bonner, K Jones, EA Emms, F Leeson, PD Marwood, R Patel, S Patel, S Rowley, M Thomas, S Carling, RW
Citation
Kw. Moore et al., 4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D-4 receptors, BIOORG MED, 9(9), 1999, pp. 1285-1290
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
9
Year of publication
1999
Pages
1285 - 1290
Database
ISI
SICI code
0960-894X(19990503)9:9<1285:4PDWHA>2.0.ZU;2-K
Abstract
The syntheses of a number of different N-linked heterocyclic pyrazole repla cements based on the structure 1 are described (compounds 3-12) as hD4 liga nds. After further optimisation the best compound identified was 13 which h as high affinity for hD4 (5.2 nM) and >300-fold selectivity for hD4 recepto rs over hD2 and hD3 receptors. (C) 1999 Elsevier Science Ltd. All rights re served.