Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

Sturino, Claudio F; O'Neill, Gary; Lachance, Nicolas; Boyd, Michael; Berthelette, Carl; Labelle, Marc; Li, Lianhai; Roy, Bruno; Scheigetz, John; Tsou, Nancy; Aubin, Yves; Bateman, Kevin P; Chauret, Nathalie; Day, Stephen H; Lévesque, Jean-François; Seto, Carmai; Silva, Jose H; Trimble, Laird A; Carriere, Marie-Claude; Denis, Danielle; Greig, Gillian; Kargman, Stacia; Lamontagne, Sonia; Mathieu, Marie-Claude; Sawyer, Nicole; Slipetz, Deborah; Abraham, William M; Jones, Tom; McAuliffe, Malia; Piechuta, Hana; Nicoll-Griffith, Deborah A; Wang, Zhaoyin; Zamboni, Robert; Young, Robert N; Metters, Kathleen M

Sturino, Claudio F; O'Neill, Gary; Lachance, Nicolas; Boyd, Michael; Berthelette, Carl; Labelle, Marc; Li, Lianhai; Roy, Bruno; Scheigetz, John; Tsou, Nancy; Aubin, Yves; Bateman, Kevin P; Chauret, Nathalie; Day, Stephen H; Lévesque, Jean-François; Seto, Carmai; Silva, Jose H; Trimble, Laird A; Carriere, Marie-Claude; Denis, Danielle; Greig, Gillian; Kargman, Stacia; Lamontagne, Sonia; Mathieu, Marie-Claude; Sawyer, Nicole; Slipetz, Deborah; Abraham, William M; Jones, Tom; McAuliffe, Malia; Piechuta, Hana; Nicoll-Griffith, Deborah A; Wang, Zhaoyin; Zamboni, Robert; Young, Robert N; Metters, Kathleen M.

Sturino CF; Department of Medicinal Chemistry, Merck Frosst Canada & Co., 16711 Trans Canada Highway, Kirkland, Quebec H9H 3L1, Canada. claudio_sturino@merck.com

J Med Chem ; 50(4): 794-806, 2007 Feb 22.

Article en En | MEDLINE | ID: mdl-17300164

Asunto(s)

Indoles/síntesis química; Receptores Inmunológicos/antagonistas & inhibidores; Receptores de Prostaglandina/antagonistas & inhibidores; Obstrucción de las Vías Aéreas/tratamiento farmacológico; Animales; Bilis/metabolismo; Unión Competitiva; Perros; Hepatocitos/metabolismo; Humanos; Técnicas In Vitro; Indoles/farmacocinética; Indoles/farmacología; Macaca fascicularis; Masculino; Ratones; Microsomas/metabolismo; Descongestionantes Nasales/síntesis química; Descongestionantes Nasales/farmacocinética; Descongestionantes Nasales/farmacología; Unión Proteica; Ratas; Ratas Sprague-Dawley; Ovinos; Estereoisomerismo; Relación Estructura-Actividad

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Banco de datos: MEDLINE Asunto principal: Receptores de Prostaglandina / Receptores Inmunológicos / Indoles Límite: Animals / Humans / Male Idioma: En Año: 2007 Tipo del documento: Article

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