Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377391 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
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).
Graphical abstractThe identification of a novel series of 1,3,4-oxadiazoles is described. The SAR of the series was explored and led to the identification of the most potent compound in the series, compound 5b with a binding pIC50 value of 8.6 (IC50 2.5 nM) and a FLIPR pKi value of 8.2 (Ki 6.3 nM).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Adrian Hall, Susan H. Brown, Anita Chowdhury, Gerard M.P. Giblin, Mairi Gibson, Mark P. Healy, David G. Livermore, Richard J. McArthur Wilson, Alan Naylor, D. Anthony Rawlings, Shilina Roman, Emma Ward, Caroline Willay,