Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands
David J Rawson1, Delphine Brugier, Anthony Harrison
1Sandwich Laboratories, Pfizer Global Research and Development, Sandwich, Kent, UK. david.rawson@pfizer.com
Bioorganic & Medicinal Chemistry Letters
|May 10, 2011
Abstract:
Conformational constraint has been used to design a potent series of α(2)δ 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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