Title of article
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists
Author/Authors
Adrian Hall، نويسنده , , Susan H. Brown، نويسنده , , Anita Chowdhury، نويسنده , , Gerard M.P. Giblin، نويسنده , , Mairi Gibson، نويسنده , , Mark P. Healy، نويسنده , , David G. Livermore، نويسنده , , Richard J. McArthur Wilson، نويسنده , , Alan Naylor، نويسنده , , D. Anthony Rawlings، نويسنده , , Shilina Roman، نويسنده , , Emma Ward، نويسنده , , Caroline Willay، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
4450
To page
4455
Abstract
A novel series of oxadiazole EP1 receptor antagonists was identified by replacing the amide of a known glycine sulfonamide derivative with a 1,3,4-oxadiazole. Optimization of the substitution patterns on the three aromatic rings led to the identification of high affinity EP1 receptor antagonists. The derivative with highest affinity displayed a binding IC50 of 2.5 nM (pIC50 8.6).
Keywords
Amide isostere , EP1 antagonist , Oxadiazole
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798441
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