Synthesis, modelling and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors

…, L Ciranna, J Alvarez-Builla, R Alajarin…

Index: Gitto, Rosaria; De Luca, Laura; Ferro, Stefania; Russo, Emilio; De Sarro, Giovambattista; Chisari, Mariangela; Ciranna, Lucia; Alvarez-Builla, Julio; Alajarin, Ramon; Buemi, Maria Rosa; Chimirri, Alba Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 3 p. 1040 - 1048

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Citation Number: 6

Abstract

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 ...