title: Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.
abstract: A number of 4'-heterocyclic biphenylsulfonamide derivatives, formally derived from BMS-193884 (1) by replacing the oxazole ring with other heterocyclic rings, are potent and selective endothelin A (ET(A)) receptor antagonists. Among the analogues examined, the pyrimidine derivative 18 is the most potent (K(i)=0.9 nM) and selective for the ET(A) receptor, approximately equivalent to 1.
authors.affiliation: Department of Chemistry, Cardiovascular Agents, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-5400, USA. natesan.murugesan@bms.com
authors.forename: Natesan
authors.initials: N
authors.lastname: Murugesan
authors.forename: Zhengxiang
authors.initials: Z
authors.lastname: Gu
authors.forename: Philip D
authors.initials: PD
authors.lastname: Stein
authors.forename: Steven
authors.initials: S
authors.lastname: Spergel
authors.forename: Sharon
authors.initials: S
authors.lastname: Bisaha
authors.forename: Eddie C-K
authors.initials: EC
authors.lastname: Liu
authors.forename: Rongan
authors.initials: R
authors.lastname: Zhang
authors.forename: Maria L
authors.initials: ML
authors.lastname: Webb
authors.forename: Suzanne
authors.initials: S
authors.lastname: Moreland
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
mesh_terms: D000818:Animals; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016466:CHO Cells; D006224:Cricetinae; D065128:Endothelin Receptor Antagonists; D006801:Humans; D011485:Protein Binding; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014162:Transfection
chemical_list: D001713:Biphenyl Compounds; D065128:Endothelin Receptor Antagonists; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin; D013449:Sulfonamides