Title of article
Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
1213
To page
1216
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794163
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