Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

Authors
Witherington, J Bordas, V Cooper, DG Forbes, IT Gribble, AD Ife, RJ Berkhout, T Gohil, J Groot, PHE
Citation
J. Witherington et al., Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists, BIOORG MED, 11(16), 2001, pp. 2177-2180
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
16
Year of publication
2001
Pages
2177 - 2180
Database
ISI
SICI code
0960-894X(20010820)11:16<2177:CRIDAP>2.0.ZU;2-Z
Abstract
The preparation and biological evaluation of a series of indolopiperidine C CR2B receptor antagonists possessing a conformationally restricted C-5 link er chain in combination with a restricted piperidine ring are described. Co mpared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors. (C) 2001 E lsevier Science Ltd. All rights reserved.