Part 3: Design and synthesis of proline-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:
A potent series of substituted (2S,4S)-benzylproline α(2)δ ligands have been designed from the readily available starting material (2S,4R)-hydroxy-L-proline. The ligands have improved pharmacokinetic profile over the (4S)-phenoxyproline derivatives described previously and have potential for development as oral agents for the treatment of neuropathic pain. Compound 16 has been progressed to clinical development.
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