title: Bis-sulfonamides as endothelin receptor antagonists.
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.
authors.affiliation: Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH-4123 Allschwil/BL, Switzerland. christoph.boss@actelion.com
authors.forename: Christoph
authors.initials: C
authors.lastname: Boss
authors.forename: Martin H
authors.initials: MH
authors.lastname: Bolli
authors.forename: Thomas
authors.initials: T
authors.lastname: Weller
authors.forename: Walter
authors.initials: W
authors.lastname: Fischli
authors.forename: Martine
authors.initials: M
authors.lastname: Clozel
mesh_terms: D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D016466:CHO Cells; D006224:Cricetinae; D065128:Endothelin Receptor Antagonists; D006801:Humans; D020128:Inhibitory Concentration 50; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D051381:Rats; D017466:Receptors, Endothelin / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology*; D014661:Vasoconstriction / Q000187:drug effects
chemical_list: D065128:Endothelin Receptor Antagonists; D017466:Receptors, Endothelin; D013449:Sulfonamides