Author/Authors :
Brian E. Kornberg، نويسنده , , Sham S. Nikam، نويسنده , , Jon L. Wright، نويسنده , , Suzanne R. Kesten، نويسنده , , Leonard T. Meltzer، نويسنده , , Linda Coughenour، نويسنده , , Bridget Barr، نويسنده , , Kevin A. Serpa، نويسنده , , Julie McCormick، نويسنده ,
Abstract :
A benzylpiperidine analogue with an acetylenic linker, 5-{3-[4-(4-fluorobenzyl)-piperidin-1-yl]-prop-1-ynyl}-1,3-dihydrobenzimidazol-2-one (3), was identified as a chemical lead with excellent activity at the NR1A/2B receptor (IC50=3 nM). Efforts to optimize this activity led to focused modifications around the structural motif of 3. The synthesis and SAR studies are discussed.
