4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase

Éva Bokor, Sándor Kun, Tibor Docsa, Pál Gergely, László Somsák

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Inhibition of glycogen phosphorylases may lead to pharmacological treatments of diseases in which glycogen metabolism plays an important role: first of all in diabetes, but also in cardiovascular and tumorous disorders. C-(β-d-Glucopyranosyl) isoxazole, pyrazole, thiazole, and imidazole type compounds were synthesized, and the latter showed the strongest inhibition against rabbit muscle glycogen phosphorylase b. Most efficient was 2-(β-d-glucopyranosyl)-4(5)-(2-naphthyl)-imidazole (11b, Ki = 31 nM) representing the best nanomolar glucose derived inhibitor of the enzyme.

Original languageEnglish
Pages (from-to)1215-1219
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume6
Issue number12
DOIs
Publication statusPublished - Dec 10 2015

Keywords

  • C-Glucopyranosyl derivative
  • glycogen phosphorylase
  • imidazole
  • inhibitor
  • isoxazole
  • pyrazole
  • thiazole

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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