Synthesis and in vivo evaluation of bicyclic gababutins

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 α2δ and were profiled in an in vivo model of neuropathic pain.

A range of bicyclic gababutins were synthesised. Of these compounds (−)-(11A) and (20A) proved to have excellent levels of in vitro potency and were profiled in an in vivo model of neuropathic pain.Figure optionsDownload as PowerPoint slide