N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

Jason M. Elliott,Robert W. Carling,Mark Chambers,Gary G. Chicchi,Peter H. Hutson, A. Brian Jones, Angus MacLeod, Rose Marwood,Georgina Meneses-Lorente, Elena Mezzogori,Fraser Murray,Michael Rigby, Inmaculada Royo,Michael G.N. Russell,Bindi Sohal,Kwei Lan Tsao,Brian Williams

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

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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