Design, total synthesis, and biological evaluation of neodysiherbaine A derivative as potential probes

Makoto Sasaki, Koichi Tsubone, Muneo Shoji, Masato Oikawa, Keiko Shimamoto, Ryuichi Sakai

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

To enable studies to elucidate the detailed biological function of dysiherbaine and neodysiherbaine A, potent and subunit-selective agonists for ionotropic glutamate receptors, the derivative with a hydroxymethyl substituent at the C10 position has been developed. Preliminary biological evaluation of the analogue showed that a C10 hydroxymethyl substituent produced significant alterations in binding affinities for the ionotropic glutamate receptor subtypes.

Original languageEnglish
Pages (from-to)5784-5787
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number22
DOIs
Publication statusPublished - 2006 Nov 15

Keywords

  • AMPA receptors
  • Dysiherbaine
  • Excitatory amino acid
  • Glutamate receptors
  • Kainate receptors
  • Neodysiherbaine A
  • Total synthesis

ASJC Scopus subject areas

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

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