| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370836 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Conformational constraint has been used to design a potent series of α2δ ligands derived from the readily available starting material (2S,4R)-hydroxy-l-proline. The ligands have improved physicochemistry and potency compared to their linear counterparts (described in our earlier publication) and the lead compound has been progressed to clinical development.
Graphical abstractA series of proline-derived α2δ ligands has been designed through cyclisation of a lead series of N-alkylated glycines. Excellent levels of potency have been achieved and compound 18 has been progressed to clinical development.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David J. Rawson, Delphine Brugier, Anthony Harrison, Jo Hough, Julie Newman, Joe Otterburn, Graham N. Maw, Jenny Price, Lisa R. Thompson, Paul Turnpenny, Andrew N. Warren,