Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-kaitocephalin

Bioorg Med Chem Lett. 2009 Jan 1;19(1):132-5. doi: 10.1016/j.bmcl.2008.11.004. Epub 2008 Nov 6.

Abstract

The design and synthesis of four pyrrolidine scaffolds that are structurally related to the known ionotropic glutamate receptor antagonist, (-)-kaitocephalin, is described. Additionally, preliminary results of the biological evaluation of these compounds are disclosed.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Design
  • Excitatory Amino Acid Agonists / chemistry
  • Excitatory Amino Acid Antagonists / chemistry
  • Humans
  • Ligands
  • Pyrroles / chemistry*
  • Pyrrolidines / chemical synthesis*
  • Pyrrolidines / pharmacology
  • Receptors, Glutamate / drug effects*
  • Structure-Activity Relationship

Substances

  • Excitatory Amino Acid Agonists
  • Excitatory Amino Acid Antagonists
  • Ligands
  • Pyrroles
  • Pyrrolidines
  • Receptors, Glutamate
  • kaitocephalin