1.
J Med Chem
; 51(13): 3946-52, 2008 Jul 10.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18553956
RESUMO
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.
Assuntos
Aminas/química , Benzofenonas/química , Benzofenonas/farmacologia , Antagonistas de Receptor B1 da Bradicinina , Animais , Benzofenonas/síntese química , Linhagem Celular , Cães , Humanos , Estrutura Molecular , Ratos , Receptor B1 da Bradicinina/metabolismo , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 17(11): 3006-9, 2007 Jun 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17428657
RESUMO
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.