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Discovery and Optimization of a Novel Class of Orally Active Nonpeptidic Endothelin-A Receptor Antagonists

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journal contribution
posted on 24.05.1996, 00:00 by Hartmut Riechers, Hans-Peter Albrecht, Willi Amberg, Ernst Baumann, Harald Bernard, Hans-Joachim Böhm, Dagmar Klinge, Andreas Kling, Stefan Müller, Manfred Raschack, Liliane Unger, Nigel Walker, Wolfgang Wernet
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 compounds are endothelin-A-selective, are orally available, and show a long duration of action.