title: 2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.
abstract: A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent, cross-species active, and functional urotensin-II receptor antagonists such as 1a and 11a are described.
authors.affiliation: Cardiovascular and Urogenital Center of Excellence for Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA. jian.jin@gsk.com
authors.forename: Jian
authors.initials: J
authors.lastname: Jin
authors.forename: Yonghui
authors.initials: Y
authors.lastname: Wang
authors.forename: Feng
authors.initials: F
authors.lastname: Wang
authors.forename: Dongchuan
authors.initials: D
authors.lastname: Shi
authors.forename: Karl F
authors.initials: KF
authors.lastname: Erhard
authors.forename: Zining
authors.initials: Z
authors.lastname: Wu
authors.forename: Brian F
authors.initials: BF
authors.lastname: Guida
authors.forename: Sarah K
authors.initials: SK
authors.lastname: Lawrence
authors.forename: David J
authors.initials: DJ
authors.lastname: Behm
authors.forename: Jyoti
authors.initials: J
authors.lastname: Disa
authors.forename: Kalindi S
authors.initials: KS
authors.lastname: Vaidya
authors.forename: Christopher
authors.initials: C
authors.lastname: Evans
authors.forename: Lynette J
authors.initials: LJ
authors.lastname: McMillan
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Rivero
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Neeb
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Douglas
mesh_terms: D001665:Binding Sites; D006801:Humans; D008744:Methylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D008956:Models, Chemical; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014662:Vasoconstrictor Agents / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D008744:Methylamines; D010880:Piperidines; D043562:Receptors, G-Protein-Coupled; C121697:UTS2R protein, human; D014662:Vasoconstrictor Agents