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Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists |
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| Authors: | Charles J. McIntyre John A. McCauley Bohumil Bednar Rodney A. Bednar John W. Butcher David A. Claremon Michael E. Cunningham Roger M. Freidinger Stanley L. Gaul Carl F. Homnick Ken S. Koblan Scott D. Mosser Joseph J. Romano Nigel J. Liverton |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA;2. Department of Molecular Pharmacology, Merck Research Laboratories, West Point, PA 19486, USA |
| Abstract: | A novel series of annulated tricyclic compounds was synthesized and evaluated as NMDA/NR2B antagonists. Structure–activity development was directed towards in vitro optimization of NR2B activity and selectivity over the hERG K+ channel. Preferred compounds were subsequently evaluated for selectivity in an α1-adrenergic receptor binding counter-screen and a cell-based assay of NR2B activity. |
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