title: 5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.
abstract: A series of 2,3-diaminopyridine bradykinin B(1) antagonists was modified to mitigate the potential for bioactivation. Removal of the 3-amino group and incorporation of basic 5-piperazinyl carboxamides at the pyridine 5-position provided compounds with high affinity for the human B(1) receptor.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com
authors.forename: Scott D
authors.initials: SD
authors.lastname: Kuduk
authors.forename: Christina Ng
authors.initials: CN
authors.lastname: Di Marco
authors.forename: Ronald K
authors.initials: RK
authors.lastname: Chang
authors.forename: Michael R
authors.initials: MR
authors.lastname: Wood
authors.forename: June J
authors.initials: JJ
authors.lastname: Kim
authors.forename: Kathy M
authors.initials: KM
authors.lastname: Schirripa
authors.forename: Kathy L
authors.initials: KL
authors.lastname: Murphy
authors.forename: Richard W
authors.initials: RW
authors.lastname: Ransom
authors.forename: Cuyue
authors.initials: C
authors.lastname: Tang
authors.forename: Maricel
authors.initials: M
authors.lastname: Torrent
authors.forename: Sookhee
authors.initials: S
authors.lastname: Ha
authors.forename: Thomayant
authors.initials: T
authors.lastname: Prueksaritanont
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: Mark G
authors.initials: MG
authors.lastname: Bock
mesh_terms: D065169:Bradykinin B1 Receptor Antagonists; D006801:Humans; D008958:Models, Molecular; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D065169:Bradykinin B1 Receptor Antagonists; D010879:Piperazines