Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0] octane derivative.

As part of a research program aiming at the design, synthesis and pharmacol ogical evaluation of a novel lead-candidates of neuroactive compounds, we d escribe herein the synthesis and the central profile of a new nebracetam an alog having a 2-aza-bicyclo[ 3.3.0] octane system. The new derivative, desi gned on the basis of the conformational restriction concept, was synthesize d in good yields exploring a diastereoselective reductive-amination and cyc lization one-pot sequence. The pharmacological profile of this new compound , investigated by using path-clamp techniques on neurons of the CNS, indica ted no effects on these cells.