Title of article
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849
Author/Authors
David R. Witty، نويسنده , , John H. Bateson، نويسنده , , Guillaume J. Hervieu، نويسنده , , Phillip Jeffrey، نويسنده , , Christopher N. Johnson، نويسنده , , Alison I. Muir، نويسنده , , Peter J. O’Hanlon، نويسنده , , Geoffrey Stemp، نويسنده , , Alex J. Stevens، نويسنده , , Kevin M. Thewlis، نويسنده , , Shelagh Wilson، نويسنده , , Kim Y. Winborn، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
7
From page
4865
To page
4871
Abstract
We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were utilised to allow rapid exploration of the structure–activity relationship around this template, leading to compound SB-568849 which possessed good receptor affinity and selectivity. This compound proved to be an antagonist with stability in vivo, an acceptable brain–blood ratio and oral bioavailability.
Keywords
Antagonist , Melanin-concentrating hormone , obesity , feeding , stress , Anxiety , MCH , Biphenylcarboxamide , MCH R1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797296
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