Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations |
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| Authors: | V Kumar PM Carabateas JA Dority WG Earley JP Mallamo C Subramanyam LD Aimone B Ault DL DeHaven Hudkins MS Miller |
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| Affiliation: | Department of Medicinal Chemistry, Sterling Winthrop Pharmaceuticals Research Division, Collegeville, Pennsylvania 19426-0900, USA. |
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| Abstract: | Replacement of the pyridinium ring of 6,11-ethanobenzob]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. |
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