Bis-sulfonamides as endothelin receptor antagonists |
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| Authors: | Boss Christoph Bolli Martin H Weller Thomas Fischli Walter Clozel Martine |
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| Institution: | Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH-4123 Allschwil/BL, Switzerland. christoph.boss@actelion.com |
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| Abstract: | Modification of the structure of bosentan 1, the first marketed endothelin receptor antagonist (Tracleer), by introduction of a second sulfonamide function at the alkoxy side chain, led to bis-sulfonamides 2. This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the pharmacological consequences of selective ET(B) receptor blockade. |
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