Document Report Card

ID: ALA1128370

Journal: J Med Chem

Title: Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations.

Authors: Kumar V, Carabateas PM, Dority JA, Earley WG, Mallamo JP, Subramanyam C, Aimone LD, Ault B, DeHaven Hudkins DL, Miller MS.

Abstract: Replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with thiazolium (4a and 4b) and N-methylimidazolium (4c and 4d) resulted in equipotent compounds in the [3H]TCP binding assay. The corresponding N-methyl-1,2,4-triazolium analogs were less potent in this assay. The thiazolium derivative 4b, with a Ki = 2.9 nM, is being evaluated as a possible neuroprotective N-methyl-D-aspartic acid (NMDA) antagonist.

CiteXplore: 7752207

DOI: 10.1021/jm00010a028