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 HUDKINS DLD MILLER MS
Citation
V. Kumar et al., NOVEL NMDA ANTAGONISTS - REPLACEMENT OF THE PYRIDINIUM RING OF 6,11-ETHANOBENZO[B]QUINOLIZINIUM CATIONS WITH HETEROISOQUINOLINIUM CATIONS, Journal of medicinal chemistry, 38(10), 1995, pp. 1826-1830
Citations number
19
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
38
Issue
10
Year of publication
1995
Pages
1826 - 1830
Database
ISI
SICI code
0022-2623(1995)38:10<1826:NNA-RO>2.0.ZU;2-2
Abstract
Replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with thiazolium (4a and 4b) and N-methylimidazolium (4c and 4 d) resulted in equipotent compounds in the [H-3]TCP binding assay. The corresponding N-methyl-1,2,4-triazolium analogs were less potent in t his assay. The thiazolium derivative 4b, with a K-i = 2.9 nM, is being evaluated as a possible neuroprotective N-methyl-D-aspartic acid (NMD A) antagonist.