1,3-disubstituted-2-carboxy quinolones: Highly potent and selective endothelin A receptor antagonists

Authors
Haesslein, JL Baholet, I Fortin, M Iltis, A Khider, J Periers, AM Pierre, C Vevert, JP
Citation
Jl. Haesslein et al., 1,3-disubstituted-2-carboxy quinolones: Highly potent and selective endothelin A receptor antagonists, BIOORG MED, 10(13), 2000, pp. 1487-1490
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
13
Year of publication
2000
Pages
1487 - 1490
Database
ISI
SICI code
0960-894X(20000703)10:13<1487:1QHPAS>2.0.ZU;2-B
Abstract
The design, synthesis, and in vitro biological activity of a series of 2-ca rboxy quinolone antagonists selective for the endothelin A receptor are pre sented. Introduction of a second acid group in position 3 of the quinolone ring increases dramatically the selectivity for ETA. (C) 2000 Elsevier Scie nce Ltd. All rights reserved.