| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376305 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
A high-throughput screen targeting the EP1 receptor identified non-acidic glycine sulfonamide derivative 2a with a pKi of 6.2. Analogue synthesis allowed a thorough investigation of the structure–activity relationship (SAR) and led to a 100-fold increase in recombinant potency.
Graphical abstractThe discovery, synthesis, pharmacokinetic profile and structure–activity relationships of a novel series of non-acidic EP1 receptor antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Stephen C. McKeown, Adrian Hall, Richard Blunt, Susan H. Brown, Iain P. Chessell, Anita Chowdhury, Gerard M.P. Giblin, Mark P. Healy, Matthew R. Johnson, Olivier Lorthioir, Anton D. Michel, Alan Naylor, Xiao Lewell, Shilina Roman, Stephen P. Watson,