title: Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.
abstract: We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models.
authors.affiliation: Department of Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, MS 29-1-B, Thousand Oaks, CA 91320, USA.
authors.forename: Kaustav
authors.initials: K
authors.lastname: Biswas
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Aya
authors.forename: Wenyuan
authors.initials: W
authors.lastname: Qian
authors.forename: Tanya A N
authors.initials: TA
authors.lastname: Peterkin
authors.forename: Jian Jeffrey
authors.initials: JJ
authors.lastname: Chen
authors.forename: Jason
authors.initials: J
authors.lastname: Human
authors.forename: Randall W
authors.initials: RW
authors.lastname: Hungate
authors.forename: Gondi
authors.initials: G
authors.lastname: Kumar
authors.forename: Leyla
authors.initials: L
authors.lastname: Arik
authors.forename: Dianna
authors.initials: D
authors.lastname: Lester-Zeiner
authors.forename: Gloria
authors.initials: G
authors.lastname: Biddlecome
authors.forename: Barton H
authors.initials: BH
authors.lastname: Manning
authors.forename: Hong
authors.initials: H
authors.lastname: Sun
authors.forename: Hong
authors.initials: H
authors.lastname: Dong
authors.forename: Ming
authors.initials: M
authors.lastname: Huang
authors.forename: Richard
authors.initials: R
authors.lastname: Loeloff
authors.forename: Eileen J
authors.initials: EJ
authors.lastname: Johnson
authors.forename: Benny C
authors.initials: BC
authors.lastname: Askew
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology; D065169:Bradykinin B1 Receptor Antagonists; D065094:Bradykinin B2 Receptor Antagonists; D002908:Chronic Disease; D006801:Humans; D010146:Pain / Q000188:drug therapy*; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D013450:Sulfones / Q000008:administration & dosage / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D065169:Bradykinin B1 Receptor Antagonists; D065094:Bradykinin B2 Receptor Antagonists; D013450:Sulfones