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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3771-3. doi: 10.1016/j.bmcl.2011.04.058. Epub 2011 Apr 20.

Part 3: Design and synthesis of proline-derived α2δ ligands.

Author information

1
Sandwich Laboratories, Pfizer Global Research and Development, Sandwich, Kent, UK. david.rawson@pfizer.com

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.

PMID:
21550802
DOI:
10.1016/j.bmcl.2011.04.058
[Indexed for MEDLINE]

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