Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands

Abstract Conformational constraint has been used to design a potent series of α 2 δ ligands derived from the readily available starting material (2 S ,4 R )-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.