Kumar V, Carabateas P M, Dority J A, Earley W G, Mallamo J P, Subramanyam C, Aimone L D, Ault B, DeHaven Hudkins D L, Miller M S
Department of Medicinal Chemistry, Sterling Winthrop Pharmaceuticals Research Division, Collegeville, Pennsylvania 19426-0900, USA.
J Med Chem. 1995 May 12;38(10):1826-30. doi: 10.1021/jm00010a028.
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.
将6,11-亚乙基苯并[b]喹啉鎓阳离子的吡啶环用噻唑鎓（4a和4b）和N-甲基咪唑鎓（4c和4d）取代，在[3H]TCP结合试验中得到了等效的化合物。相应的N-甲基-1,2,4-三唑鎓类似物在该试验中的活性较低。噻唑鎓衍生物4b的Ki = 2.9 nM，正在作为一种可能的神经保护性N-甲基-D-天冬氨酸（NMDA）拮抗剂进行评估。
