2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.
Selective bradykinin (BK) B 1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compound 1 provided potent hBK B 1 receptor antagonists with excellent receptor occupancy in the CNS of hBK B 1 transgenic rats.
Su
Dai-Shi
DS
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. daishi_su@merck.com
Lim
John L
JL
Tinney
Elizabeth
E
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
Yu
Jian
J
Tang
Cuyue
C
Prueksaritanont
Thomayant
T
Freidinger
Roger M
RM
Bock
Mark G
MG
Anthony
Neville J
NJ
D000588:Amines / Q000737:chemistry*; D000818:Animals; D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D065169:Bradykinin B1 Receptor Antagonists; D002460:Cell Line; D004285:Dogs; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D043783:Receptor, Bradykinin B1 / Q000378:metabolism; D013329:Structure-Activity Relationship
D000588:Amines; D001577:Benzophenones; D065169:Bradykinin B1 Receptor Antagonists; D043783:Receptor, Bradykinin B1