Title of article
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping
Author/Authors
Adrian Hall، نويسنده , , Andy Billinton، نويسنده , , Susan H. Brown، نويسنده , , Anita Chowdhury، نويسنده , , Gerard M.P. Giblin، نويسنده , , Paul Goldsmith، نويسنده , , David N. Hurst، نويسنده , , Alan Naylor، نويسنده , , Sadhana Patel، نويسنده , , Tiziana Scoccitti، نويسنده , , Pamela J. Theobald، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
7
From page
2684
To page
2690
Abstract
We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.
Keywords
EP1 antagonist , pain , conformational constraint , Scaffold hopping , Lead hopping
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799431
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