Conformationally-restricted ligands for the histamine H-1 receptor

Authors
Upton, C Osborne, RH Jaffar, M
Citation
C. Upton et al., Conformationally-restricted ligands for the histamine H-1 receptor, BIOORG MED, 10(11), 2000, pp. 1277-1279
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
11
Year of publication
2000
Pages
1277 - 1279
Database
ISI
SICI code
0960-894X(20000605)10:11<1277:CLFTHH>2.0.ZU;2-2
Abstract
Potent H-1-antagonistic activity in a series of novel indeno[2,1-c]pyridine s and their 4-arylpiperidinol precursors is reported; one compound shows an in vitro activity four times that of the standard mepyramine that it was s creened against. Their Failure to translate this protection to in vivo test s is discussed. (C) 2000 Elsevier Science Ltd. All rights reserved.