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

Jamie L. Cohen, Agenor Limon-Ruiz, Ricardo Miledi, A. Richard Chamberlin

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

The design and synthesis of four 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate-containing natural products, including (-)-dysiherbaine, is described. Biological evaluation of these analogs shows that one is a KA receptor antagonist and another is an NMDA receptor agonist.

Original languageEnglish (US)
Pages (from-to)2189-2194
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number8
DOIs
StatePublished - Apr 15 2006
Externally publishedYes

Fingerprint

N-Methyl-D-Aspartate Receptors
Biological Products
Scaffolds
Glutamic Acid
Ligands
dysiherbaine

Keywords

  • Dysiherbaine
  • Excitatory amino acid receptors
  • KA receptor agonist
  • KA reeptor antagonist
  • NMDA receptor agonist
  • Scaffold

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine. / Cohen, Jamie L.; Limon-Ruiz, Agenor; Miledi, Ricardo; Chamberlin, A. Richard.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 8, 15.04.2006, p. 2189-2194.

Research output: Contribution to journalArticle

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