2,3-diaminopyridine bradykinin B1 receptor antagonists.
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.
Kuduk
Scott D
SD
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, Pennsylvania 19486, USA. scott_d_kuduk@merck.com
Ng
Christina
C
Feng
Dong-Mei
DM
Wai
Jenny M-C
JM
Chang
Raymond S L
RS
Harrell
Charles M
CM
Murphy
Kathy L
KL
Ransom
Richard W
RW
Reiss
Duane
D
Ivarsson
Magnus
M
Mason
Glenn
G
Boyce
Susan
S
Tang
Cuyue
C
Prueksaritanont
Thomayant
T
Freidinger
Roger M
RM
Pettibone
Douglas J
DJ
Bock
Mark G
MG
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
D000631:Aminopyridines; D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D065169:Bradykinin B1 Receptor Antagonists; C038615:2,3-diaminopyridine