2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.
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.
Feng
Dong-Mei
DM
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. dongmei_feng@merck.com
Wai
Jenny M
JM
Kuduk
Scott D
SD
Ng
Christina
C
Murphy
Kathy L
KL
Ransom
Richard W
RW
Reiss
Duane
D
Chang
Raymond S L
RS
Harrell
Charles M
CM
MacNeil
Tanya
T
Tang
Cuyue
C
Prueksaritanont
Thomayant
T
Freidinger
Roger M
RM
Pettibone
Douglas J
DJ
Bock
Mark G
MG
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
D000631:Aminopyridines; D065169:Bradykinin B1 Receptor Antagonists; D011725:Pyridines; C038615:2,3-diaminopyridine