Jo Hough

Publications (2)5.3 Total impact

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

  David J Rawson, Delphine Brugier, Anthony Harrison, Jo Hough, Julie Newman, Joe Otterburn, Graham N Maw, Jenny Price, Lisa R Thompson, Paul Turnpenny, Andrew N Warren
  [show abstract] [hide abstract]
  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.
  Bioorganic & medicinal chemistry letters 06/2011; 21(12):3771-3. · 2.65 Impact Factor
• Article: Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands.

  David J Rawson, Delphine Brugier, Anthony Harrison, Jo Hough, Julie Newman, Joe Otterburn, Graham N Maw, Jenny Price, Lisa R Thompson, Paul Turnpenny, Andrew N Warren
  [show abstract] [hide abstract]
  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.
  Bioorganic & medicinal chemistry letters 06/2011; 21(12):3767-70. · 2.65 Impact Factor