Title of article
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions
Author/Authors
Ho-Jane Shue، نويسنده , , Xiao Chen، نويسنده , , John H. Schwerdt، نويسنده , , Sunil Paliwal، نويسنده , , David J. Blythin، نويسنده , , Ling Lin، نويسنده , , Danlin Gu، نويسنده , , Cheng Wang، نويسنده , , Gregory A. Reichard، نويسنده , , Hongwu Wang، نويسنده , , John J. Piwinski، نويسنده , , Ruth A. Duffy، نويسنده , , Jean E. Lachowicz، نويسنده , , Vicki L. Coffin، نويسنده , , Amin A. Nomeir، نويسنده , , Cynthia A. Morgan، نويسنده , , Geoffrey B. Varty، نويسنده , , Neng-Yang Shih، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
1065
To page
1069
Abstract
A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an α-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.
Keywords
Improved potency , NK1 antagonist , Sustained in vivo activity
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796519
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