title: Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
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 compounds are endothelin-A-selective, are orally available, and show a long duration of action.
authors.affiliation: Hauptlaboratorium, BASF AG, Ludwigshafen, Germany.
authors.forename: H
authors.initials: H
authors.lastname: Riechers
authors.forename: H P
authors.initials: HP
authors.lastname: Albrecht
authors.forename: W
authors.initials: W
authors.lastname: Amberg
authors.forename: E
authors.initials: E
authors.lastname: Baumann
authors.forename: H
authors.initials: H
authors.lastname: Bernard
authors.forename: H J
authors.initials: HJ
authors.lastname: Böhm
authors.forename: D
authors.initials: D
authors.lastname: Klinge
authors.forename: A
authors.initials: A
authors.lastname: Kling
authors.forename: S
authors.initials: S
authors.lastname: Müller
authors.forename: M
authors.initials: M
authors.lastname: Raschack
authors.forename: L
authors.initials: L
authors.lastname: Unger
authors.forename: N
authors.initials: N
authors.lastname: Walker
authors.forename: W
authors.initials: W
authors.lastname: Wernet
mesh_terms: D000284:Administration, Oral; D000818:Animals; D003619:Dansyl Compounds / Q000494:pharmacology; D003645:Death, Sudden; D015195:Drug Design; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000037:antagonists & inhibitors / Q000633:toxicity*; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology; D000096926:Benzenesulfonamides
chemical_list: D003619:Dansyl Compounds; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D008024:Ligands; D011743:Pyrimidines; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin; D013449:Sulfonamides; C083751:Ro 46-2005; D000096926:Benzenesulfonamides; C085754:5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide