2-aryl indole NK1 receptor antagonists: Optimisation of the 2-aryl ring and the indole nitrogen substituent

Authors
Dinnell, K Chicchi, GG Dhar, MJ Elliott, JM Hollingworth, GJ Kurtz, MM Ridgill, MP Rycroft, W Tsao, KL Williams, AR Swain, CJ
Citation
K. Dinnell et al., 2-aryl indole NK1 receptor antagonists: Optimisation of the 2-aryl ring and the indole nitrogen substituent, BIOORG MED, 11(9), 2001, pp. 1237-1240
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
9
Year of publication
2001
Pages
1237 - 1240
Database
ISI
SICI code
0960-894X(20010507)11:9<1237:2INRAO>2.0.ZU;2-T
Abstract
Novel 2-aryl indole hNK(1) receptor ligands were prepared utilising palladi um cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK(1) receptor binding affinity and good brain penetration (e.g ., 9d) were synthesised. (C) 2001 Elsevier Science Ltd. All rights reserved .