C-glucopyranosyl-1,2,4-triazoles as new potent inhibitors of glycogen phosphorylase

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Abstract

Glycogen phosphorylase inhibitors are considered as potential antidiabetic agents. 3-(β-d-Glucopyranosyl)-5-substituted-1,2,4-triazoles were prepared by acylation of O-perbenzoylated N1-tosyl-C-β-d-glucopyranosyl formamidrazone and subsequent removal of the protecting groups. The best inhibitor was 3-(β-d-glucopyranosyl)-5-(2-naphthyl)-1,2,4-triazole (K i = 0.41 μM against rabbit muscle glycogen phosphorylase b).

Original languageEnglish
Pages (from-to)612-615
Number of pages4
JournalACS Medicinal Chemistry Letters
Volume4
Issue number7
DOIs
Publication statusPublished - Jul 11 2013

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Keywords

  • 1,2,4-Triazole
  • C-glucopyranosyl derivative
  • bioisoster
  • glycogen phosphorylase
  • inhibitor

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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