title: Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.
abstract: Selective bradykinin (BK) B(1) receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure-activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B(1) receptor antagonists.
authors.affiliation: Department of Medicinal Chemistry, West Point, PA 19486, USA. daishi_su@merck.com
authors.forename: Dai-Shi
authors.initials: DS
authors.lastname: Su
authors.forename: John L
authors.initials: JL
authors.lastname: Lim
authors.forename: M Kristine
authors.initials: MK
authors.lastname: Markowitz
authors.forename: Bang-Lin
authors.initials: BL
authors.lastname: Wan
authors.forename: Kathy L
authors.initials: KL
authors.lastname: Murphy
authors.forename: Duane R
authors.initials: DR
authors.lastname: Reiss
authors.forename: C Meacham
authors.initials: CM
authors.lastname: Harrell
authors.forename: Stacy S
authors.initials: SS
authors.lastname: O'Malley
authors.forename: Rick W
authors.initials: RW
authors.lastname: Ransom
authors.forename: Raymond S L
authors.initials: RS
authors.lastname: Chang
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: Cuyue
authors.initials: C
authors.lastname: Tang
authors.forename: Thomayant
authors.initials: T
authors.lastname: Prueksaritanont
authors.forename: Roger M
authors.initials: RM
authors.lastname: Freidinger
authors.forename: Mark G
authors.initials: MG
authors.lastname: Bock
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D030801:Animals, Genetically Modified; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D065169:Bradykinin B1 Receptor Antagonists; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D043783:Receptor, Bradykinin B1 / Q000235:genetics; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D065169:Bradykinin B1 Receptor Antagonists; D003510:Cyclohexanes; D006845:Hydrocarbons, Fluorinated; D011725:Pyridines; D043783:Receptor, Bradykinin B1