Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.
Basic Information
ID: ALA1155351
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.
Authors: McIntyre CJ, McCauley JA, Bednar B, Bednar RA, Butcher JW, Claremon DA, Cunningham ME, Freidinger RM, Gaul SL, Homnick CF, Koblan KS, Mosser SD, Romano JJ, Liverton NJ.
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 alpha(1)-adrenergic receptor binding counter-screen and a cell-based assay of NR2B activity.
CiteXplore: 19648007
DOI: 10.1016/j.bmcl.2009.07.028
Patent ID: ┄