,4-DIARYL-2-OXO-1,2-DIHYRDO-QUINOLINE-3-CARBOXYLIC ACIDS AS ENDOTHELIN RECEPTOR ANTAGONISTS

Authors
MEDERSKI WWKR OSSWALD M DORSCH D CHRISTADLER M SCHMITGES CJ WILM C
Citation
Wwkr. Mederski et al., ,4-DIARYL-2-OXO-1,2-DIHYRDO-QUINOLINE-3-CARBOXYLIC ACIDS AS ENDOTHELIN RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 7(14), 1997, pp. 1883-1886
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
14
Year of publication
1997
Pages
1883 - 1886
Database
ISI
SICI code
0960-894X(1997)7:14<1883:,AAE>2.0.ZU;2-A
Abstract
The discovery, synthesis and structure-activity relationships of a ser ies of novel ,4-diaryl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids as non-selective endothelin ETA/ETB receptor antagonists are described . The most potent inhibitor 3m displayed an IC50 of 260 nM and 200 nM for ETA and ETB receptors,respectively. (C) 1997 Elsevier Science Ltd.