DISCOVERY AND OPTIMIZATION OF A NOVEL CLASS OF ORALLY-ACTIVE NONPEPTIDIC ENDOTHELIN-A RECEPTOR ANTAGONISTS

Authors
RIECHERS H ALBRECHT HP AMBERG W BAUMANN E BERNARD H BOHM HJ KLINGE D KLING A MULLER S RASCHACK M UNGER L WALKER N WERNET W
Citation
H. Riechers et al., DISCOVERY AND OPTIMIZATION OF A NOVEL CLASS OF ORALLY-ACTIVE NONPEPTIDIC ENDOTHELIN-A RECEPTOR ANTAGONISTS, Journal of medicinal chemistry, 39(11), 1996, pp. 2123-2128
Citations number
26
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
39
Issue
11
Year of publication
1996
Pages
2123 - 2128
Database
ISI
SICI code
0022-2623(1996)39:11<2123:DAOOAN>2.0.ZU;2-J
Abstract
A novel class of endothelin-A receptor ligands was discovered by high- throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compoun ds are endothelin-A-selective, are orally available, and show a long d uration of action.