Synthesis and in vivo evaluation of 3,4-disubstituted gababutins

A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against α2δ and was profiled in in vivo models of pain and anxiety.

A range of 3,4-disubstituted gababutins were synthesised and, of these, the stand-out compound was (21). This compound was profiled in in vivo models of pain and anxiety.Figure optionsDownload as PowerPoint slide