Abstract A three-step synthetic pathway has been employed to synthesize a small library of 2- (4-arylpiperidin-1-yl)-1-(1H-indol-3-yl) ethanone and 2-(4-arylpiperidin-1-yl)-1-(1H-indol-3- yl) ethane-1, 2-dione derivatives that have been screened in [3 H] ifenprodil competition binding assay. Some compounds exhibited significant binding affinity at nanomolar concentration, the most active being ligand 35 (IC 50= 5.5 nM). Docking experiments ...