Synthesis and in vivo evaluation of 3-substituted gababutins

A range of 3-alkylated five-membered ring derivatives of Gabapentin were synthesized and several were found to have good levels of potency against the α2δ calcium subunit of a voltage-gated calcium channel. Two compounds were profiled in in vivo models of pain and anxiety.

A range of 3-alkylated five-membered ring derivatives of Gabapentin were synthesized and several were found to have superior potency against the α2δ calcium subunit. Diastereoisomeric compounds, (16) and (22), were profiled in in vivo models of pain and anxiety and proved to have different levels of efficacy in the two models.Figure optionsDownload as PowerPoint slide