title: 2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.
abstract: A novel class of 2,3-diaminopyridine bradykinin B1 receptor antagonists is disclosed. Structure-activity relationship studies (SARs) that led to compounds with significantly improved potency and pharmacokinetic properties relative to the lead compound are described.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. dongmei_feng@merck.com
authors.forename: Dong-Mei
authors.initials: DM
authors.lastname: Feng
authors.forename: Jenny M
authors.initials: JM
authors.lastname: Wai
authors.forename: Scott D
authors.initials: SD
authors.lastname: Kuduk
authors.forename: Christina
authors.initials: C
authors.lastname: Ng
authors.forename: Kathy L
authors.initials: KL
authors.lastname: Murphy
authors.forename: Richard W
authors.initials: RW
authors.lastname: Ransom
authors.forename: Duane
authors.initials: D
authors.lastname: Reiss
authors.forename: Raymond S L
authors.initials: RS
authors.lastname: Chang
authors.forename: Charles M
authors.initials: CM
authors.lastname: Harrell
authors.forename: Tanya
authors.initials: T
authors.lastname: MacNeil
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: Douglas J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: Mark G
authors.initials: MG
authors.lastname: Bock
mesh_terms: D000631:Aminopyridines / Q000737:chemistry / Q000494:pharmacology*; D065169:Bradykinin B1 Receptor Antagonists; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000631:Aminopyridines; D065169:Bradykinin B1 Receptor Antagonists; D011725:Pyridines; C038615:2,3-diaminopyridine