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

  • Bioorg Med Chem Lett. 1999 Jun 7;9(11):1619-24. doi: 10.1016/s0960-894x(99)00248-6.
A P Tamiz  1 ,  E R Whittemore ,  R M Woodward ,  R B Upasani ,  J F Keana
Affiliations
  • 1. Department of Chemistry, University of Oregon, Eugene 97403, USA.
PMID: 10386947 DOI: 10.1016/s0960-894x(99)00248-6
Abstract

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.