title: Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].
abstract: On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl]amine] had analgesic activity in the rat.
authors.affiliation: Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. robin.clark5@verizon.net
authors.forename: Robin D
authors.initials: RD
authors.lastname: Clark
authors.forename: Alam
authors.initials: A
authors.lastname: Jahangir
authors.forename: Daniel
authors.initials: D
authors.lastname: Severance
authors.forename: Rick
authors.initials: R
authors.lastname: Salazar
authors.forename: Thomas
authors.initials: T
authors.lastname: Chang
authors.forename: David
authors.initials: D
authors.lastname: Chang
authors.forename: Mary Frances
authors.initials: MF
authors.lastname: Jett
authors.forename: Steven
authors.initials: S
authors.lastname: Smith
authors.forename: Keith
authors.initials: K
authors.lastname: Bley
mesh_terms: D000284:Administration, Oral; D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D001682:Biological Availability; D002351:Carrageenan / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006801:Humans; D006930:Hyperalgesia / Q000139:chemically induced / Q000188:drug therapy; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D051381:Rats; D044006:Receptors, Epoprostenol / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000814:Aniline Compounds; D007093:Imidazoles; D044006:Receptors, Epoprostenol; C000622556:Ro 1138452; D002351:Carrageenan