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.

Afiliación

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 en 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.

Asunto(s)

Aminas/química; Benzofenonas/química; Benzofenonas/farmacología; Antagonistas del Receptor de Bradiquinina B1; Animales; Benzofenonas/síntesis química; Línea Celular; Perros; Humanos; Estructura Molecular; Ratas; Receptor de Bradiquinina B1/metabolismo; Relación Estructura-Actividad

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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Benzofenonas / Antagonistas del Receptor de Bradiquinina B1 / Aminas Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2008 Tipo del documento: Article

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