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

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Abstract

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.

Graphical abstract

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.

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Acknowledgements

We would like to thank Jane McGuffog for GC/HPLC analysis and Giles Ratcliffe for NMR studies.

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