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N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
Elliott, Jason M; Carling, Robert W; Chambers, Mark; Chicchi, Gary G; Hutson, Peter H; Jones, A Brian; MacLeod, Angus; Marwood, Rose; Meneses-Lorente, Georgina; Mezzogori, Elena; Murray, Fraser; Rigby, Michael; Royo, Inmaculada; Russell, Michael G N; Sohal, Bindi; Tsao, Kwei Lan; Williams, Brian.
Afiliação
  • Elliott JM; Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. jason@elliottj25.fsnet.co.uk
Bioorg Med Chem Lett ; 16(22): 5748-51, 2006 Nov 15.
Article em En | MEDLINE | ID: mdl-16950620
A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properties.
Assuntos
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinolinas / Receptores da Neurocinina-3 / Neurotransmissores / Hidrazinas Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2006 Tipo de documento: Article
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinolinas / Receptores da Neurocinina-3 / Neurotransmissores / Hidrazinas Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2006 Tipo de documento: Article
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