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.
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. daishi_su@merck.com
Dai-Shi
DS
Su
John L
JL
Lim
Elizabeth
E
Tinney
Bang-Lin
BL
Wan
Kathy L
KL
Murphy
Duane R
DR
Reiss
C Meacham
CM
Harrell
Stacy S
SS
O'Malley
Rick W
RW
Ransom
Raymond S L
RS
Chang
Douglas J
DJ
Pettibone
Jian
J
Yu
Cuyue
C
Tang
Thomayant
T
Prueksaritanont
Roger M
RM
Freidinger
Mark G
MG
Bock
Neville J
NJ
Anthony
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