Part 2: Design, synthesis and evaluation of hydroxyproline-derived α₂δ ligands
2011
Rawson, David J. | Brugier, Delphine | Harrison, Anthony | Hough, Jo | Newman, Julie | Otterburn, Joe | Maw, Graham N. | Price, Jenny | Thompson, Lisa R. | Turnpenny, Paul | Warren, Andrew N.
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.
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