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

Éva Bokor, Sándor Kun, T. Docsa, P. Gergely, L. 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

Fingerprint

Imidazoles
Glycogen Phosphorylase
Phosphorylase b
Isoxazoles
Thiazoles
Glucose
Enzyme Inhibitors
Medical problems
Glycogen
Metabolism
Muscle
Pharmacology
Rabbits
Muscles
imidazole
pyrazole

Keywords

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

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

Cite this

4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase. / Bokor, Éva; Kun, Sándor; Docsa, T.; Gergely, P.; Somsák, L.

In: ACS Medicinal Chemistry Letters, Vol. 6, No. 12, 10.12.2015, p. 1215-1219.

Research output: Contribution to journalArticle

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