1.
Bioorg Med Chem Lett
; 14(5): 1213-6, 2004 Mar 08.
Artigo
em Inglês
| MEDLINE
| ID: mdl-14980668
RESUMO
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.