title: 2,3-diaminopyridine bradykinin B1 receptor antagonists.
abstract: Bradykinin B1 receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. A series of 2,3-diaminopyridine B1 antagonists was optimized to have sub-nanomolar affinity and good pharmacokinetic properties. Lead compounds were shown to exhibit good efficacy in rabbit in vivo models of pain and inflammation.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, Pennsylvania 19486, USA. scott_d_kuduk@merck.com
authors.forename: Scott D
authors.initials: SD
authors.lastname: Kuduk
authors.forename: Christina
authors.initials: C
authors.lastname: Ng
authors.forename: Dong-Mei
authors.initials: DM
authors.lastname: Feng
authors.forename: Jenny M-C
authors.initials: JM
authors.lastname: Wai
authors.forename: Raymond S L
authors.initials: RS
authors.lastname: Chang
authors.forename: Charles M
authors.initials: CM
authors.lastname: Harrell
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: Magnus
authors.initials: M
authors.lastname: Ivarsson
authors.forename: Glenn
authors.initials: G
authors.lastname: Mason
authors.forename: Susan
authors.initials: S
authors.lastname: Boyce
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 / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D065169:Bradykinin B1 Receptor Antagonists; D004285:Dogs; D006207:Half-Life; D007249:Inflammation / Q000188:drug therapy; D010147:Pain Measurement; D011817:Rabbits; D051381:Rats; D013045:Species Specificity; D013329:Structure-Activity Relationship
chemical_list: D000631:Aminopyridines; D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D065169:Bradykinin B1 Receptor Antagonists; C038615:2,3-diaminopyridine