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Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Scott, Jack D; Miller, Michael W; Li, Sarah W; Lin, Sue-Ing; Vaccaro, Henry A; Hong, Liwu; Mullins, Deborra E; Guzzi, Mario; Weinstein, Jay; Hodgson, Robert A; Varty, Geoffrey B; Stamford, Andrew W; Chan, Tin-Yau; McKittrick, Brian A; Greenlee, William J; Priestley, Tony; Parker, Eric M.
Afiliación
  • Scott JD; Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jack.scott@spcorp.com
Bioorg Med Chem Lett ; 19(21): 6018-22, 2009 Nov 01.
Article en En | MEDLINE | ID: mdl-19800231
Vasopressin 1b (V1b) antagonists have been postulated as possible treatments for depression and anxiety. A novel series of potent and selective V1b antagonists has been identified starting from an in-house screen hit. The incorporation of a sulfonamide linker between a tetrahydroisoquinoline core and amino piperidine lead to the identification of a V1b antagonist with similar affinity for human and rat receptors. Further optimization of the right hand portion afforded potent V1b antagonists that possessed moderate to high selectivity over other receptors.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinolinas / Sulfonamidas / Fármacos Antidiuréticos / Antagonistas de los Receptores de Hormonas Antidiuréticas Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinolinas / Sulfonamidas / Fármacos Antidiuréticos / Antagonistas de los Receptores de Hormonas Antidiuréticas Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido