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

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

A potent series of substituted (2S,4S)-benzylproline α₂δ 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 developme...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-06, Vol.21 (12), p.3771-3773
Hauptverfasser: 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
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Biological and medical sciences
chemistry
Drug Design
Humans
Inhibitory Concentration 50
Ligands
Medical sciences
Miscellaneous
Molecular Structure
Neuropharmacology
Pain
pharmacokinetics
Pharmacology. Drug treatments
Proline - chemical synthesis
Proline - chemistry
Proline - pharmacology
Rats
Swine
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Zusammenfassung:A potent series of substituted (2S,4S)-benzylproline α₂δ 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.04.058