Title of article
N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II
Author/Authors
Jason M. Elliott، نويسنده , , Robert W. Carling، نويسنده , , Gary G. Chicchi، نويسنده , , James Crawforth، نويسنده , , Peter H. Hutson، نويسنده , , A. Brian Jones، نويسنده , , Sarah Kelly، نويسنده , , Rose Marwood، نويسنده , , Georgina Meneses-Lorente، نويسنده , , Elena Mezzogori، نويسنده , , Fraser Murray، نويسنده , , Michael Rigby، نويسنده , , Inmaculada ROYO، نويسنده , , Michael G.N. Russell، نويسنده , , Duncan Shaw، نويسنده , , Bindi Sohal، نويسنده , , Kwei-Lan Tsao، نويسنده , , Brian Williams، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5752
To page
5756
Abstract
Introduction of selected amine containing side chains into the 3-position of N′,2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted hPXR activation. Introduction of a fluorine at the 8-position is necessary to minimize unwanted hIKr affinity and a piperazine N-tert-butyl group is necessary for metabolic stability. The lead compound (8m) occupies receptors within the CNS following oral dosing (Occ90 7 mg/kg po; plasma Occ90 0.4 μM) and has good selectivity and excellent PK properties.
Keywords
NK3 , Schizophrenia , N?-2-Diphenylquinoline-4-carbohydrazide
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797467
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