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N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Elliott JM,Carling RW,Chambers M,Chicchi GG,Hutson PH,Jones AB,MacLeod A,Marwood R,Meneses-Lorente G,Mezzogori E,Murray F,Rigby M,Royo I,Russell MG,Sohal B,Tsao KL,Williams B

doi

10.1016/j.bmcl.2006.08.086

subject

Has Abstract

pub_date

2006-11-15 00:00:00

pages

5748-51

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00987-5

journal_volume

16

pub_type

杂志文章

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