Title of article
From arylureas to biarylamides to aminoquinazolines: Discovery of a novel, potent TRPV1 antagonist
Author/Authors
Xiaozhang Zheng، نويسنده , , Kevin J. Hodgetts، نويسنده , , Harry Brielmann، نويسنده , , Alan Hutchison، نويسنده , , Frank Burkamp، نويسنده , , A. Brian Jones، نويسنده , , Peter Blurton، نويسنده , , Robert Clarkson، نويسنده , , Jayaraman Chandrasekhar، نويسنده , , Rajagopal Bakthavatchalam، نويسنده , , Stéphane De Lombaert، نويسنده , , Marci Crandall، نويسنده , , Daniel Cortright، نويسنده , , Charles A. Blum، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5217
To page
5221
Abstract
Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. The development of B-ring SAR led to the conformationally constrained analog 70. The resulting aminoquinazoline 70 represents a novel VR1 antagonist with improved in vitro potency and oral bioavailability vs the analogous compounds from the lead series.
Keywords
pain , Ureas , Bioisostere , Antagonist , TRPV1 , VR1 , Quinazoline
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797360
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