Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors

Tamiz, A.P.; Whittemore, E.R.; Woodward, R.M.; Upasani, R.B.; Keana, J.F.

Bioorganic and Medicinal Chemistry Letters 9(11): 1619-1624


ISSN/ISBN: 0960-894X
PMID: 10386947
DOI: 10.1016/s0960-894x(99)00248-6
Accession: 047458679

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A series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles was synthesized as potential antagonists for the NR1A/2B subtype of N-methyl-D-aspartate (NMDA) receptors. Assayed by electrical recording under steady-state conditions, 7-hydroxy-2-(4-phenylbutyl)- 1,2,3,4-tetrahydropyrido-[3,4-b]indole (30) was the most potent compound in the series having an IC50 value of 50 nM at the NR1A/2B receptors.