title: The design and synthesis of a novel series of indole derived selective ET(A) antagonists.
abstract: Conformational constraint has been used as the key design element in the identification of a series of potent and selective ET(A) antagonists. The most potent antagonist, 32, (ET(A) IC(50)=0.55nM) is 722-fold selective over the ET(B) receptor, as measured by binding experiments.
authors.affiliation: Department of Discovery Chemistry, Pfizer Central Research, Sandwich, Kent CT13 9NJ, UK. david_rawson@sandwich.pfizer.com
authors.forename: David J
authors.initials: DJ
authors.lastname: Rawson
authors.forename: Kevin N
authors.initials: KN
authors.lastname: Dack
authors.forename: Roger P
authors.initials: RP
authors.lastname: Dickinson
authors.forename: Kim
authors.initials: K
authors.lastname: James
mesh_terms: D065128:Endothelin Receptor Antagonists; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D044022:Receptor, Endothelin A; D013329:Structure-Activity Relationship
chemical_list: D065128:Endothelin Receptor Antagonists; D007211:Indoles; D044022:Receptor, Endothelin A