5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.
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.
Kuduk
Scott D
SD
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com
Di Marco
Christina Ng
CN
Chang
Ronald K
RK
Wood
Michael R
MR
Kim
June J
JJ
Schirripa
Kathy M
KM
Murphy
Kathy L
KL
Ransom
Richard W
RW
Tang
Cuyue
C
Torrent
Maricel
M
Ha
Sookhee
S
Prueksaritanont
Thomayant
T
Pettibone
Douglas J
DJ
Bock
Mark G
MG
D065169:Bradykinin B1 Receptor Antagonists; D006801:Humans; D008958:Models, Molecular; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*
D065169:Bradykinin B1 Receptor Antagonists; D010879:Piperazines