Selective alpha(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

Authors
Nantermet, PG Barrow, JC Selnick, HG Homnick, CF Freidinger, RM Chang, RSL O'Malley, SS Reiss, DR Broten, TP Ransom, RW Pettibone, DJ Olah, T Forray, C
Citation
Pg. Nantermet et al., Selective alpha(1a) adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones, BIOORG MED, 10(15), 2000, pp. 1625-1628
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
15
Year of publication
2000
Pages
1625 - 1628
Database
ISI
SICI code
0960-894X(20000807)10:15<1625:SAARAB>2.0.ZU;2-7
Abstract
A series of alpha(1a) receptor antagonists derived from a 4-aryl-3,4-dihydr opyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to p icomolar range along with high selectivity was obtained. In vivo efficacy i n a prostate contraction model in rats was observed with a few derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.