Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.
Selective bradykinin (BK) B(1) receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure-activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B(1) receptor antagonists.
Su
Dai-Shi
DS
Department of Medicinal Chemistry, West Point, PA 19486, USA. daishi_su@merck.com
Lim
John L
JL
Markowitz
M Kristine
MK
Wan
Bang-Lin
BL
Murphy
Kathy L
KL
Reiss
Duane R
DR
Harrell
C Meacham
CM
O'Malley
Stacy S
SS
Ransom
Rick W
RW
Chang
Raymond S L
RS
Pettibone
Douglas J
DJ
Tang
Cuyue
C
Prueksaritanont
Thomayant
T
Freidinger
Roger M
RM
Bock
Mark G
MG
D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D030801:Animals, Genetically Modified; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D065169:Bradykinin B1 Receptor Antagonists; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D043783:Receptor, Bradykinin B1 / Q000235:genetics; D013329:Structure-Activity Relationship
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D065169:Bradykinin B1 Receptor Antagonists; D003510:Cyclohexanes; D006845:Hydrocarbons, Fluorinated; D011725:Pyridines; D043783:Receptor, Bradykinin B1