1.
J Med Chem
; 51(13): 3946-52, 2008 Jul 10.
Article
in English
| MEDLINE
| ID: mdl-18553956
ABSTRACT
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.
Subject(s)
Amines/chemistry , Benzophenones/chemistry , Benzophenones/pharmacology , Bradykinin B1 Receptor Antagonists , Animals , Benzophenones/chemical synthesis , Cell Line , Dogs , Humans , Molecular Structure , Rats , Receptor, Bradykinin B1/metabolism , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 17(11): 3006-9, 2007 Jun 01.
Article
in English
| MEDLINE
| ID: mdl-17428657
ABSTRACT
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.