2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Su, Dai-Shi; Lim, John L; Tinney, Elizabeth; Wan, Bang-Lin; Murphy, Kathy L; Reiss, Duane R; Harrell, C Meacham; O'Malley, Stacy S; Ransom, Rick W; Chang, Raymond S L; Pettibone, Douglas J; Yu, Jian; Tang, Cuyue; Prueksaritanont, Thomayant; Freidinger, Roger M; Bock, Mark G; Anthony, Neville J

Su, Dai-Shi; Lim, John L; Tinney, Elizabeth; Wan, Bang-Lin; Murphy, Kathy L; Reiss, Duane R; Harrell, C Meacham; O'Malley, Stacy S; Ransom, Rick W; Chang, Raymond S L; Pettibone, Douglas J; Yu, Jian; Tang, Cuyue; Prueksaritanont, Thomayant; Freidinger, Roger M; Bock, Mark G; Anthony, Neville J.

Afiliação

Su DS; Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. daishi_su@merck.com

J Med Chem ; 51(13): 3946-52, 2008 Jul 10.

Article em En | MEDLINE | ID: mdl-18553956

ABSTRACT

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.

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

Texto completo

Imprimir

XML

PubMed Links

Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzofenonas / Antagonistas de Receptor B1 da Bradicinina / Aminas Limite: Animals / Humans Idioma: En Ano de publicação: 2008 Tipo de documento: Article

Texto completo

Imprimir

XML

PubMed Links

Buscar no Google