Synthesis and in vivo evaluation of bicyclic gababutins

  • Bioorg Med Chem Lett. 2010 Jan 15;20(2):461-4. doi: 10.1016/j.bmcl.2009.11.118.
David C Blakemore  1 ,  Justin S Bryans ,  Pauline Carnell ,  Christopher L Carr ,  Nicola E A Chessum ,  Mark J Field ,  Natasha Kinsella ,  Simon A Osborne ,  Andrew N Warren ,  Sophie C Williams
Affiliations
  • 1. Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. [email protected]
PMID: 20005103 DOI: 10.1016/j.bmcl.2009.11.118
Abstract

Synthesis of a number of bicyclic five-membered ring derivatives of gabapentin led to the identification of two compounds, (-)-(11A) and (20A) which both had an excellent level of potency against alpha(2)delta and were profiled in an in vivo model of neuropathic pain.