Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.

Burgey, Christopher S; Robinson, Kyle A; Lyle, Terry A; Sanderson, Philip E J; Lewis, S Dale; Lucas, Bobby J; Krueger, Julie A; Singh, Rominder; Miller-Stein, Cynthia; White, Rebecca B; Wong, Bradley; Lyle, Elizabeth A; Williams, Peter D; Coburn, Craig A; Dorsey, Bruce D; Barrow, James C; Stranieri, Maria T; Holahan, Marie A; Sitko, Gary R; Cook, Jacquelynn J; McMasters, Daniel R; McDonough, Colleen M; Sanders, William M; Wallace, Audrey A; Clayton, Franklin C; Bohn, Dennis; Leonard, Yvonne M; Detwiler, Theodore J; Lynch, Joseph J; Yan, Youwei; Chen, Zhongguo; Kuo, Lawrence; Gardell, Stephen J; Shafer, Jules A; Vacca, Joseph P

Burgey, Christopher S; Robinson, Kyle A; Lyle, Terry A; Sanderson, Philip E J; Lewis, S Dale; Lucas, Bobby J; Krueger, Julie A; Singh, Rominder; Miller-Stein, Cynthia; White, Rebecca B; Wong, Bradley; Lyle, Elizabeth A; Williams, Peter D; Coburn, Craig A; Dorsey, Bruce D; Barrow, James C; Stranieri, Maria T; Holahan, Marie A; Sitko, Gary R; Cook, Jacquelynn J; McMasters, Daniel R; McDonough, Colleen M; Sanders, William M; Wallace, Audrey A; Clayton, Franklin C; Bohn, Dennis; Leonard, Yvonne M; Detwiler, Theodore J; Lynch, Joseph J; Yan, Youwei; Chen, Zhongguo; Kuo, Lawrence; Gardell, Stephen J; Shafer, Jules A; Vacca, Joseph P.

Afiliación

Burgey CS; Departments of Medicinal Chemistry, Biological Chemistry, Drug Metabolism, Molecular Systems, Structural Biology, and Pharmacology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. christopher_burgey@merck.com

J Med Chem ; 46(4): 461-73, 2003 Feb 13.

Article en En | MEDLINE | ID: mdl-12570369

Asunto(s)

Acetamidas/farmacocinética; Anticoagulantes/farmacocinética; Inhibidores de Proteasas/síntesis química; Pirazinas/farmacocinética; Piridinas/farmacocinética; Trombina/antagonistas & inhibidores; Acetamidas/síntesis química; Acetamidas/farmacología; Administración Oral; Animales; Anticoagulantes/síntesis química; Anticoagulantes/farmacología; Disponibilidad Biológica; Cristalografía por Rayos X; Perros; Macaca mulatta; Modelos Moleculares; Inhibidores de Proteasas/química; Inhibidores de Proteasas/farmacología; Pirazinas/síntesis química; Pirazinas/farmacología; Piridinas/síntesis química; Piridinas/farmacología; Ratas; Relación Estructura-Actividad

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Bases de datos: MEDLINE Asunto principal: Inhibidores de Proteasas / Pirazinas / Piridinas / Trombina / Acetamidas / Anticoagulantes Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2003 Tipo del documento: Article País de afiliación: Estados Unidos

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