Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues |
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| Authors: | Kornberg Brian E Nikam Sham S Wright Jon L Kesten Suzanne R Meltzer Leonard T Coughenour Linda Barr Bridget Serpa Kevin A McCormick Julie |
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| Institution: | Department of Chemistry, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. brian.kornberg@pfizer.com |
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| 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. |
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