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N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists |
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| Authors: | 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 |
| Affiliation: | 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 |
| Abstract: | 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. |
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