Novel heterocycles as selective alpha(1)-adrenergic receptor antagonists

Citation
Xb. Li et al., Novel heterocycles as selective alpha(1)-adrenergic receptor antagonists, BIOORG MED, 10(20), 2000, pp. 2375-2377
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2375 - 2377
Database
ISI
SICI code
0960-894X(20001016)10:20<2375:NHASAR>2.0.ZU;2-1
Abstract
A novel series of aryl piperazine substituted heterocycles has been synthes ized and identified as antagonists of the alpha (1a) adrenergic receptor (a lpha (1a)-AR), which has been implicated in benign prostatic hyperplasia (B PH). These compounds selectively inhibit binding to the alpha (1a)-AR with K(i)s as low as 2.1 nM. (C) 2000 Elsevier Science Ltd. All rights reserved.